MedWorm.com provides a medical RSS filtering service. Over 6000 RSS medical sources are combined and output via different filters. This feed contains the latest items from the 'European Journal of Pharmaceutical Sciences' source. Wed, 08 Feb 2012 14:04:14 +0100 http://www.medworm.com/index.php?rid=5626379&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22266210%26dopt%3DAbstract Authors: Qin Y, Li Z, Chen Y, Hui H, Sun Y, Yang H, Lu N, Guo Q Abstract Flavonoid is an important group of natural products which exerted anticancer effects against various cancers. III-10 is a newly synthesized flavonoid with a pyrrolidinyl and a benzyl group substitution. It shares a same carbon skeleton with flavonoid which indicates that it may also have potential anticancer activity. To investigate whether III-10 could express anticancer effect on human U937 leukemia cells through differentiation induction, a series of experiments were processed. MTT and trypan-blue excluding assays showed that III-10 possessed growth and viability inhibition effects on U937 cells. Giemsa staining was implemented to observe the morphologic changes of U937 cells after III-10 treatment. Nitrobl... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5626379 Sun, 15 Jan 2012 05:00:00 +0100 5626379 http://www.medworm.com/index.php?rid=5626378&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22266211%26dopt%3DAbstract Authors: Li T, Chen H, Yang Z, Wei N, Zhang S, Mei X, Bai SF Abstract Pseudolaric acid B (PAB) is a novel diterpenoid, isolated from Pseudolarix kaempferi Gorden, which roots are widely used to treat inflammatory and microbial skin diseases for centuries, but the underlying mechanism remains elusive. To address the immunoregulatory mechanisms of PAB, we first investigated the effect of PAB in 2,4-dinitrofluorobenzene (DNFB)-induced contact hypersensitivity (CHS) mice. The expression of specific transcription factors for T-helper (Th)1, Th2, Th17 and regulatory T cells (Tregs) was determined by RT-PCR, and the capacities for PAB to modulate Th1/Th17/Treg cell subsets was furtherly analyzed by flow cytometric analysis, ELISA and Western blotting assay. The results showed that topical... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5626378 Sun, 15 Jan 2012 05:00:00 +0100 5626378 http://www.medworm.com/index.php?rid=5626377&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22266212%26dopt%3DAbstract Authors: Thati J, Rasmuson KC Abstract The influence of process conditions on the properties of benzoic acid spherical agglomerates, are investigated. Agglomerates are produced in a fed-batch agitated tank process. Benzoic acid is dissolved in ethanol and the solution is mixed with the bridging liquid, before being fed into an agitated aqueous solution. A broader investigation has been performed using heptane as the bridging liquid, and in further experiments different bridging liquids are compared. The results show that the bridging liquid has an influence on the product properties, with diethyl ether and ethyl acetate being at the extreme end with no agglomerates formed at all. Using any of the other five solvents (chloroform, toluene, heptane, pentane, or cyclohexane) spherical ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5626377 Sun, 15 Jan 2012 05:00:00 +0100 5626377 http://www.medworm.com/index.php?rid=5606886&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22251657%26dopt%3DAbstract Authors: Zhao P, Jiang H, Jiang T, Zhi Z, Wu C, Sun C, Zhang J, Wang S Abstract Fibrous ordered mesoporous carbon (FOMC) was developed as a new drug delivery system for loading an insoluble drug, designed to be orally administered, and then to enhance the drug loading capacity, improve the dissolution rate, enhance the oral bioavailability and reduce the gastric damage. Celecoxib (CEL) was chosen as a model drug. The nanostructures and effect of different pore sizes (4.4-7.0nm) on drug loading and release properties were studied. The results showed that FOMC has a high drug loading capacity (0.599g/g, drug weight/carrier weight) and the dissolution rate of CEL from FOMC was much faster than pure crystalline CEL using buffer (pH 6.8) as a dissolution medium. Moreover, the oral bioav... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5606886 Wed, 11 Jan 2012 05:00:00 +0100 5606886 http://www.medworm.com/index.php?rid=5606900&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22245537%26dopt%3DAbstract Authors: Doktorovova S, Shegokar R, Martins-Lopes P, Silva AM, Lopes CM, Müller RH, Souto EB Abstract Surface hydrophobicity of nanocarriers influences protein binding and subsequently fate of nanoparticles in blood circulation. Therefore, characterization of surface hydrophobicity of nanocarriers provides important preclinical information. Here, a modified classical adsorption method for the needs of characterization of cationic solid lipid nanoparticles (cSLN) was developed. We have identified possible method limitations that should be considered when performing the analysis, i.e. the problems associated with particle separation from the dispersion and their own absorbance in visible spectrum. We propose two modified methods for performing the assay overcoming the stated limitat... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5606900 Tue, 10 Jan 2012 05:00:00 +0100 5606900 http://www.medworm.com/index.php?rid=5606899&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22245538%26dopt%3DAbstract Authors: Martins S, Tho I, Souto E, Ferreira D, Brandl M Abstract Physicochemical properties of lipid nanoparticles (LN), such as size, size distribution and surface charge, have a major influence both, on in vitro stability and delivery of the incorporated drug in vivo. With the purpose of understanding how these properties are influenced by variations of LN composition (e.g. lipid and surfactant type and concentration) 2(2) factorial designs with centre point were applied for several types of lipids and surfactants in the present study. Tested factors and levels were the type and concentration of lipid (cetyl palmitate, Dynasan 114 and Witepsol E85) at the concentrations of 5%, 10% and 15%, in combination with type and concentration of surfactant (polysorbate 20, 40, 60 and 80 an... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5606899 Tue, 10 Jan 2012 05:00:00 +0100 5606899 http://www.medworm.com/index.php?rid=5606891&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22248882%26dopt%3DAbstract Authors: Zhang X, Sun M, Zheng A, Cao D, Bi Y, Sun J Abstract Poly(d,l-lactide-co-glycolide) nanoparticles (PLGA-NP) have been extensively used as a drug delivery system for proteins and peptides. However, their negative surface charge decreases bioavailability under oral administration. Recently, cationically modified PLGA-NP has been introduced as novel carriers for oral delivery. The characteristics of the nanoparticles, such as particle size, surface charge, and bioadhesion are considered the most significant determinants of the effect of these nanoparticles both in vitro and in vivo. Our aim was to introduce and evaluate the physiochemical characteristics, bioadhesion, and biological activity of positively charged chitosan-coated PLGA-NP (CS-PLGA-NP), using insulin as a model ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5606891 Tue, 10 Jan 2012 05:00:00 +0100 5606891 http://www.medworm.com/index.php?rid=5606898&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22245539%26dopt%3DAbstract In conclusion, NSAIDs with the greatest cytoprotective effect (nimesulide, celecoxib and meloxicam) may exert their effect mainly through the blockade of cyclooxygenase-2 (COX-2) activity. Other compounds with neuroprotective activity may complement their lower anti-COX-2 effect with a slight increase in interleukin 10 and reduced oxidative and nitrosative stress in our model of hypoxia-reoxygenation in rat brain slices. PMID: 22245539 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5606898 Mon, 09 Jan 2012 05:00:00 +0100 5606898 http://www.medworm.com/index.php?rid=5580136&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22234377%26dopt%3DAbstract In this study, we tested whether AN-7 protects the heart and cardiomyocytes against ischemia injury. A single oral dose of AN-7 was given to mice or rats. Animals were sacrificed 1.5 or 24h later and the hearts were subjected to ischemia and reperfusion ex-vivo (Langendorff). The mechanical performance was recorded throughout and the infarct size was measured at the end of reperfusion. Neonatal rat cardiomyocytes were subjected to 24-48h hypoxia (1% O(2)) in the absence or presence of AN-7 and mitochondria damage and cell death were assessed. Proteins were analyzed by Western immunoblotting. In the two rodents, a single dose of AN-7 given in vivo preconditioned the hearts for improved functional recovery from ischemia and reperfusion performed ex-vivo. Both 1.5h and 24h treatments improved... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5580136 Tue, 03 Jan 2012 05:00:00 +0100 5580136 http://www.medworm.com/index.php?rid=5580138&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22226647%26dopt%3DAbstract Authors: Sturzu A, Sheikh S, Klose U, Echner H, Kalbacher H, Deeg M, Nägele T, Horger M, Schwentner C, Ernemann U, Heckl S Abstract The use of tissue-specific receptor ligands is a promising approach for cancer diagnostics and therapy. Lorglumide, a highly effective competitive ligand for the cholecystokinine-A receptor (CCKRA) was conjugated to a fluorescent dye and a magnetic resonance imaging (MRI) contrast agent to obtain a bifunctional marker for tissue with high CCKRA expression. An intermediate conjugate containing only lorglumide and a fluorescent dye was also produced. By performing CCKRA mRNA expression analysis on carcinoma cell lines we found that CCKRA is highly expressed in PC3 prostate carcinoma cells compared to U373 glioma and U2OS osteosarcoma cells. Uptake, spec... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5580138 Fri, 30 Dec 2011 05:00:00 +0100 5580138 http://www.medworm.com/index.php?rid=5580137&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22227305%26dopt%3DAbstract In this study we analyzed molecular mechanisms involved in the antimigratory and antiangiogenic activity of this hydroxy anthraquinone in colon cancer cell, WiDr. Our results show that a relatively non toxic concentration of AE suppressed the phorbol-12-myristyl-13-acetate (PMA) induced migration and invasion of tumor cells. On analysis for the molecules involved in the migration/invasion, we found AE downregulated mRNA expression and promoter/gelatinolytic activity of Matrix Metalloproteinase (MMP)-2/9, as well as the RhoB expression at gene and protein level. It was also a strong inhibitor of Vascular Endothelial Growth Factor (VEGF) expression, promoter activity and endothelial cell migration/invasion and in vitro angiogenesis. AE suppressed the nuclear translocation and DNA binding of ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5580137 Fri, 30 Dec 2011 05:00:00 +0100 5580137 http://www.medworm.com/index.php?rid=5567327&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22214813%26dopt%3DAbstract Authors: Hallifax D, Turlizzi E, Zanelli U, Houston JB Abstract Underprediction of in vivo intrinsic clearance (CLint) from suspended human hepatocytes has recently been shown to be clearance-dependent although the mechanistic basis is currently unknown. One possible explanation is rate limiting transmembrane (passive) permeation into hepatocytes in vitro; evidence to support this has been minor to date, but there has not been a systematic exploration of the impact of passive permeability in vitro. To investigate the relationship between underprediction of in vivo CLint and potentially rate limiting permeability, permeability constants (Px, collated from published studies and determined experimentally in this study), using three alternative methodologies (parallel artificial membra... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5567327 Sat, 24 Dec 2011 05:00:00 +0100 5567327 http://www.medworm.com/index.php?rid=5567328&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22207039%26dopt%3DAbstract Authors: Lecoeur M, Vérones V, Vaccher C, Bonte JP, Lebegue N, Goossens JF Abstract 1-(4-Methoxyphenylethyl)-11H-benzo[f]-1,2-dihydro-pyrido[3,2,c][1,2,5]oxathiazepine 5,5 dioxide (BZN) is a cytotoxic derivative with very promising in vitro activity. Regulatory authority for registration of pharmaceuticals for human use requires to evaluate the stability of active compound under various stress conditions. Forced degradation of BZN was investigated under hydrolytic (0.1M NaOH, 0.1M HCl, neutral), oxidative (3.3% H(2)O(2)), photolytic (visible light) and thermal (25°C, 70°C) settings. Relevant degradation took place under thermal acidic (0.1M HCl, 70°C) and oxidative (3.3% H(2)O(2)) conditions. Liquid chromatography-mass spectrometry (LC-MS) analyses revealed the presence of ten ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5567328 Tue, 20 Dec 2011 05:00:00 +0100 5567328 http://www.medworm.com/index.php?rid=5552733&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22198311%26dopt%3DAbstract Authors: Fuchs H, Runge F, Held HD Abstract Linagliptin is a selective, competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, recently approved in the USA, Japan and Europe for the treatment of type 2 diabetes. It has non-linear pharmacokinetics and, unlike other DPP-4 inhibitors, a largely non-renal excretion route. It was hypothesised that P-glycoprotein (P-gp)-mediated intestinal transport could influence linagliptin bioavailability, and might contribute to its elimination. Two studies evaluated the role of P-gp-mediated transport in the bioavailability and intestinal secretion of linagliptin in rats. In the bioavailability study, male Wistar rats received single oral doses of linagliptin, 1 or 15mg/kg, plus either the P-gp inhibitor, zosuquidar trihydrochloride, or vehicle. For... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5552733 Wed, 14 Dec 2011 05:00:00 +0100 5552733 http://www.medworm.com/index.php?rid=5538188&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22186295%26dopt%3DAbstract In this study, physicochemical profiling demonstrated nano-complex formation between the PLL derivatives and siRNA (200-280nm in diameter). At physiological pH only a slight cationic surface charge (<20mV) was detected, due to the masking effect of the PEG. In contrast, significantly higher positive charges (∼20 to 30mV and >40mV) were detected upon hydrolysis of the PEG linker at acidic pHs (pH=6.8 and 5.5, respectively). The PEGylated complexes were stable in serum without significant aggregation or decomplexation of siRNA for up to 48h. At the cellular level, PEG-PLLs were comparable with the commercial carrier INTERFRin™, in terms of cellular uptake, endosomal escape and in vitro reporter gene knockdown. In vivo, utilising a mouse model grafted with prostate carcinoma, signif... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538188 Sun, 11 Dec 2011 05:00:00 +0100 5538188 http://www.medworm.com/index.php?rid=5538194&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22178292%26dopt%3DAbstract Authors: Sorokin A, Selkov G, Goryanin I Abstract The volume of the experimentally measured time series data is rapidly growing, while storage solutions offering better data types than simple arrays of numbers or opaque blobs for keeping series data are sorely lacking. A number of indexing methods have been proposed to provide efficient access to time series data, but none has so far been integrated into a tried-and-proven database system. To explore the possibility of such integration, we have developed a data type for time series storage in PostgreSQL, an object-relational database system, and equipped it with an access method based on SAX (Symbolic Aggregate Approximation). This new data type has been successfully tested in a database supporting a large-scale plant gene expressi... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538194 Fri, 09 Dec 2011 05:00:00 +0100 5538194 http://www.medworm.com/index.php?rid=5538193&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22178293%26dopt%3DAbstract Authors: Thing M, Larsen C, Ostergaard J, Jensen H, Larsen SW Abstract Most in vitro methods for evaluating parenteral oil based depots are focusing on intramuscular or subcutaneous injection. For intra-articular injection other mechanisms may control the overall drug release rate due to a relatively smaller interfacial area and longer transport distance of the drug substance in the oil to the oil-synovial fluid interface. In the current work, an in vitro model for testing drug release from oil solutions intended for intra-articular injection was evaluated. The release of the model drugs naproxen, piroxicam and ropivaciane from a well-defined surface area of the lipophilic solutions were followed using an in vitro model based on a modified USP II paddle apparatus with modest agitat... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538193 Fri, 09 Dec 2011 05:00:00 +0100 5538193 http://www.medworm.com/index.php?rid=5538190&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22178533%26dopt%3DAbstract In this study, we developed an arsenic-resistant OVCAR-3 subline (OVCAR-3/AsR) and aimed to identify the molecular mechanisms and signaling pathways contributing to the development of acquired arsenic chemoresistance in ovarian cancer. OVCAR-3/AsR cells were obtained following continual exposure of parental OVCAR-3 cells to low dose As(2)O(3) for 12months. Cytotoxicity of OVCAR-3/AsR cells to As(2)O(3), paclitaxel and cisplatin was investigated. Cell apoptosis and cell cycle distribution following As(2)O(3) treatment of OVCAR-3/AsR cells was also analyzed using flow cytometry. Subsequently, cDNA microarray analysis was performed from the RNA samples of OVCAR-3 and OVCAR-3/AsR cells in duplicate experiments. Microarray data were analyzed using Genespring® and Pathway Studio® Softwares. OV... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538190 Fri, 09 Dec 2011 05:00:00 +0100 5538190 http://www.medworm.com/index.php?rid=5538189&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22178534%26dopt%3DAbstract Authors: Klech H, Brooksbank C, Price S, Verpillat P, Bühler FR, Dubois D, Haider N, Johnson C, Lindén HH, Payton T, Renn O, See W Abstract This position paper recommends a set of standards for quality assessment of continuing professional development (CPD) for medicines research and development (R&D). We have developed these standards to help us achieve the education and training goals of the Innovative Medicines Initiative (IMI; www.imi.europa.eu/), which is developing courses to address the skills gaps in European medicines R&D. The IMI shared standard for course quality will enable professionals in medicines R&D to create a personalized portfolio of education and training that best suits their needs. Individuals already working in the pharmaceutical industry will ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538189 Fri, 09 Dec 2011 05:00:00 +0100 5538189 http://www.medworm.com/index.php?rid=5538197&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22172603%26dopt%3DAbstract Authors: Linn M, Collnot EM, Djuric D, Hempel K, Fabian E, Kolter K, Lehr CM Abstract As many new active pharmaceutical ingredients are poorly water soluble, solubility enhancers are one possibility to overcome the hurdles of drug dissolution and absorption in oral drug delivery. In the present work a novel solubility enhancing excipient (Soluplus®) was tested for its capability to improve intestinal drug absorption. BCS class II compounds danazol, fenofibrate and itraconazole were tested both in vivo in beagle dogs and in vitro in transport experiments across Caco-2 cell monolayers. Each drug was applied as pure crystalline substance, in a physical mixture with Soluplus®, and as solid solution of the drug in the excipient. In the animal studies a many fold increase in plasma AUC... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538197 Thu, 08 Dec 2011 05:00:00 +0100 5538197 http://www.medworm.com/index.php?rid=5538196&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22172604%26dopt%3DAbstract Authors: Park JH, Park JH, Hur HJ, Woo JS, Lee HJ Abstract The aims of the present study were to investigate the effects of silymarin, an inhibitor of the P-glycoprotein efflux pump, on oral bioavailability of paclitaxel in rats, and to compare pharmacokinetic parameters of paclitaxel between a commercial formulation of paclitaxel (Taxol®) and a paclitaxel microemulsion. Oral bioavailability of paclitaxel in a Taxol® formulation was enhanced in the combination with silymarin (10 and 20mg/kg). In particular, the mean maximum plasma concentration (C(max)) and the mean area under the plasma concentration-time curve (AUC(0-)(t)) of paclitaxel in the Taxol® formulation were significantly increased 3-fold and 5-fold compared with control, respectively, following oral co-administration... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538196 Thu, 08 Dec 2011 05:00:00 +0100 5538196 http://www.medworm.com/index.php?rid=5538195&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22178018%26dopt%3DAbstract This study aimed to verify the effect of Terpy and sodium nitroprusside (SNP) in basilar artery. We conducted vascular reactivity experiments on endothelium-denuded basilar rings. The concentrations of iron (Fe) and ruthenium (Ru) complex were analyzed in basilar artery lysates after incubation with NO donors by mass spectrometry. We also evaluated the NO released from SNP and Terpy by using confocal microscopy. Interestingly, Terpy did not induce relaxation of the basilar artery. SNP induced relaxation in a concentration-dependent way. NO donors cross the membrane of vascular smooth muscle and entered the cell. In spite of its permeability, Terpy did not release NO in the basilar artery. Otherwise, SNP released NO in the basilar artery cells cytoplasm. Taken together, our results demonstr... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538195 Thu, 08 Dec 2011 05:00:00 +0100 5538195 http://www.medworm.com/index.php?rid=5538192&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22178531%26dopt%3DAbstract The objective of this study was to develop novel preparation techniques for protein-loaded, controlled release alginate-poloxamer microparticles with a size range suitable for pulmonary administration. Bovine serum albumin (BSA)-loaded microparticles were prepared by spray-drying aqueous polymer-drug solutions, followed by cross-linking the particles in aqueous or ethanolic CaCl(2) or aqueous ZnSO(4) solutions. The microparticles were characterized with respect to their morphology (optical and scanning electron microscopy), particle size (laser light diffraction), calcium content (atom absorption spectroscopy), alginate content (complexation with 1,9-dimethyl methylene blue) and in vitro drug release (modified Franz diffusion cell). The spray-dried microparticles were spherical in shape wi... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538192 Thu, 08 Dec 2011 05:00:00 +0100 5538192 http://www.medworm.com/index.php?rid=5538191&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22178532%26dopt%3DAbstract Authors: Buckley ST, Fischer SM, Fricker G, Brandl M Abstract The application of in vitro models in drug permeability studies represents a useful screening tool for assessing the biopharmaceutical appropriateness of new chemical entities (NCEs). Of note, there remains an ever-increasing number of NCEs which exhibit poor aqueous solubility. However, in their classical configuration, both cellular and non-cellular in vitro models show numerous deficiencies in their ability to accurately model the absorption of such compounds. As a consequence, investigators continue to explore the possibility of modifying different experimental parameters in an attempt to yield a more bio-relevant model system which offers good compatibility with poorly soluble compounds. Moreover, in many instances ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538191 Thu, 08 Dec 2011 05:00:00 +0100 5538191 http://www.medworm.com/index.php?rid=5538198&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155747%26dopt%3DAbstract Authors: Gupta RK, Goswami DG, Singh RR, Surolia A, Panda AK Abstract Polylactide (PLA) polymer particles entrapping diphtheria toxoid (DT) or tetanus toxoid (TT) were formulated with surface coatings of soybean agglutinin to have dendritic cells (DCs) targeting ability through c-type lectin receptors (CLR). It was observed that soybean agglutinin coating resulted in more association of polymer particles with DCs. Immunization with soybean agglutinin coated polymer particles entrapping DT or TT elicited antibody response better than the plain particles entrapping antigens. Both for TT and DT, single point immunization of soybean agglutinin coated polymer particles along with alum resulted in very high antibody titers; much higher than that observed while immunizing with alum adsorb... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538198 Sun, 04 Dec 2011 05:00:00 +0100 5538198 http://www.medworm.com/index.php?rid=5538205&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155541%26dopt%3DAbstract Authors: van Rooy I, Hennink WE, Storm G, Schiffelers RM, Mastrobattista E Abstract In our previous study, phage display selections were performed by in situ perfusion of a random peptide library through a mouse brain. This yielded two peptides (GLA and GYR) that showed significant binding to human brain endothelial cells (hCMEC/D3) when displayed on phage particles, but not to human umbilical vein endothelial cells (HUVECs). In the present study, these peptides were produced synthetically and coupled to liposomes to investigate the capacity of the peptides to act as ligands for targeting to hCMEC/D3 cells. Flow cytometry studies showed that these peptides when coupled to liposomes showed weak binding to the target brain endothelial cells. We hypothesized that the weak endothelial ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538205 Sat, 03 Dec 2011 05:00:00 +0100 5538205 http://www.medworm.com/index.php?rid=5538204&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155542%26dopt%3DAbstract Authors: Chen HZ, Liu CY, Kost TA, Chao YC Abstract Budded baculovirus has become an important vector for gene delivery, vaccine development, protein expression in insect and mammalian cells, and many other emerging applications. For high-throughput applications or for long-term storage and long-distance shipping, it would be useful if the infectivity and transduction abilities of baculovirus could be maintained at room temperature under dehydrated condition. The aim of this study was to design an optimized formula that preserves the activity of baculovirus stocks during prolonged periods of dehydration at various storage temperatures. The results showed that baculovirus without any supplement rapidly lost its transduction ability after dehydration. However, of many anti-oxidants, ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538204 Sat, 03 Dec 2011 05:00:00 +0100 5538204 http://www.medworm.com/index.php?rid=5538203&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155543%26dopt%3DAbstract Authors: Ma Y, Yang Q, Wang L, Zhou X, Zhao Y, Deng Y Abstract The "accelerated blood clearance (ABC) phenomenon" of PEGylated liposomes following multiple injections has been reported recently. This immunogenicity poses a problem for research into liposomes and hinders their clinical application. However, since doxorubicin liposomes and mitoxantrone liposomes have been reported to fail to induce the ABC phenomenon, some people believe that cytotoxic drugs loaded liposomes will not produce this ABC phenomenon under multiple-dosing regimens. Nevertheless, in the present study, we report that a first injection of the PEGylated liposomal topotecan (a cell cycle-specific drug for the S phase) still produced a strong ABC phenomenon. Likewise, when the first dose of "empty" PEGylated lip... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538203 Sat, 03 Dec 2011 05:00:00 +0100 5538203 http://www.medworm.com/index.php?rid=5538202&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155544%26dopt%3DAbstract Authors: Sheihet L, Garbuzenko OB, Bushman J, Gounder MK, Minko T, Kohn J Abstract Paclitaxel (PTX) has gained widespread clinical use yet its administration is associated with significant toxicity. In the present study, the toxicity and anti-tumor efficacy of tyrosine-derived nanospheres (NSP) for the delivery of PTX was compared to a clinical formulation of PTX in PBS-diluted Cremophor® EL (PTX-CrEL-D). Maximum tolerated dose was determined using a concentration series of PTX in NSP and CrEL-D, with toxicity assessed by measuring changes in body weight. Healthy mice administered PTX-NSP continued to gain weight normally while treatment with PTX-CrEL-D resulted in significant weight loss that failed to recover following treatment. Even at the dose of 50mg/kg, PTX-NSP showed bette... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538202 Sat, 03 Dec 2011 05:00:00 +0100 5538202 http://www.medworm.com/index.php?rid=5538201&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155545%26dopt%3DAbstract Authors: Akarte AS, Srinivasan BP, Gandhi S Abstract The aim of the present study was to evaluate the relationships between the islet blood flow, nitric oxide, insulin, and cytosolic calcium in rat pancreatic islets, using dipeptidyl peptidase-IV (DPP-IV) inhibitor vildagliptin. For measuring pancreatic and islet blood a non-radioactive microsphere technique was used. Vehicle pre-treatment of glucose administered diabetic rats had decrease pancreatic and islet blood flow as compared with glucose administered normal rats. Blood glucose concentrations were not affected after vildagliptin administration in either diabetic or normal rats (10min after glucose administration). Vildagliptin had no effects on baseline pancreatic or islet blood flow in glucose administered normal rats. Admi... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538201 Sat, 03 Dec 2011 05:00:00 +0100 5538201 http://www.medworm.com/index.php?rid=5538200&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155546%26dopt%3DAbstract CONCLUSION: Exposure to 5-FU followed by cisplatin had a synergistic effect in DLD-1 cells, suggesting that the amount of platinum bound to DNA contributes to this result. Also, the effect was dependent on the type of platinum derivative and cell. PMID: 22155546 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538200 Sat, 03 Dec 2011 05:00:00 +0100 5538200 http://www.medworm.com/index.php?rid=5538199&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155547%26dopt%3DAbstract Authors: Ogungbenro K, Aarons L Abstract The aim of this paper is to assess the performance of a new mechanistic model for analysing (13)C-octanoic acid breath test data using simulation studies. The (13)C-octanoic acid breath test is widely used for indirect assessment of the rate of gastric emptying and it is yet to achieve universal acceptance due to inconsistencies when the results are compared with simultaneous and direct measurements using scintigraphy. The new semi-mechanistic model has five separate compartments; stomach, intestine, central and peripheral body and breath compartments. Stomach and breath profiles were simulated for 50 individuals under four conditions: variability on all parameters; no variability on the rate constant of gastric emptying and the rate constan... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5538199 Sat, 03 Dec 2011 05:00:00 +0100 5538199 http://www.medworm.com/index.php?rid=5478651&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22127371%26dopt%3DAbstract Authors: Matuszak N, Hamtiaux L, Baldeyroux B, Muccioli GG, Poupaert JH, Lansiaux A, Lambert DM Abstract The endocannabinoid system is implicated in numerous physiopathological processes while more and more pieces of evidence wave the link between this complex machinery and cancer related phenomenon. In these lines, we confirmed the effects of 2-arachidonoylglycerol (2-AG), the main endocannabinoid, on neuroblastoma cells proliferation in vitro, and proved that some N-phenylmaleimide compounds that were previously shown as MAGL inhibitors can also inhibit type 2 topoisomerase. We also shed light on their antiproliferative effects on a neuroblastoma cell line. In order to establish a link between MAGL inhibition, topoisomerase inhibition and the effects on N1E-115 cells, we tested c... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5478651 Wed, 23 Nov 2011 05:00:00 +0100 5478651 http://www.medworm.com/index.php?rid=5478650&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22127372%26dopt%3DAbstract This study was based on the assumption that the abrasion rate of agglomerates determines the required blending time. It is shown that the kinetic energy density of the moving powder bed is a relevant parameter which correlates with the abrasion rate of agglomerates. However, aspects related to the strength of agglomerates should also be considered. For this reason the Stokes abrasion number (St(Abr)) has been defined. This parameter describes the ratio between the kinetic energy density of the moving powder bed and the work of fracture of the agglomerate. The St(Abr) number is shown to predict the abrasion potential of agglomerates in the dry-mixing process. It appeared possible to include effects of filler particle size and impeller rotational rate into this concept. A clear relationship ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5478650 Wed, 23 Nov 2011 05:00:00 +0100 5478650 http://www.medworm.com/index.php?rid=5478653&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22119655%26dopt%3DAbstract Authors: Niu J, Su Z, Xiao Y, Huang A, Li H, Bao X, Li S, Chen Y, Sun M, Ping Q Abstract A multifunctional mixed micelle was assembled for drug targeting delivery by combining two newly synthesized amphiphilic polymers, which were octreotide-polyethylene glycol-monostearate (OPMS) and N-octyl-N-succinyl-O-carboxymethyl chitosan (OSCC), respectively. The mixed micelle was designed to be characterized with long circulation, somatostatin receptors (SSTR)-mediated endocytosis and pH sensitivity. A series of assembling proportions of OPMS and OSCC was tested to reveal the effect of compositions on the functions. The particle size, zeta potential, drug loading and critical micelle concentration were examined. The dialysis test indicated a pH-triggering release behavior of the doxorubicin... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5478653 Sun, 20 Nov 2011 05:00:00 +0100 5478653 http://www.medworm.com/index.php?rid=5478652&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22120645%26dopt%3DAbstract Authors: Mazák K, Noszál B Abstract The complete set of experimental microscopic partition coefficients of morphine was determined for the first time for any compound. The acid-base microequilibria were characterized by combining pH-potentiometry and deductive methods using auxiliary compounds of reduced complexity. The results show around three times as many non-charged than zwitterionic microspecies in aqueous solution. Partition of the individual microspecies was mimicked by model compounds of the closest possible similarity, then correction factors were determined and introduced. Thus the intrinsic partition coefficients of all the microspecies could be quantitated, including the non-charged and the zwitterionic ones. The non-charged microspecies is 1070 times as lipophilic a... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5478652 Fri, 18 Nov 2011 05:00:00 +0100 5478652 http://www.medworm.com/index.php?rid=5478657&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22115865%26dopt%3DAbstract We report a specific, fast and feasible method for the simultaneous determination of methyl mesilate (MMS), ethyl mesilate (EMS), isopropyl mesilate (IMS), methyl besilate (MBS) and ethyl besilate (EBS) in finished drug products by GC/MS. Sample preparation was carried out by liquid extraction. The analytes were directly injected into the chromatographic system and quantified with the internal standard method using methyl tosylate (MTS) as internal standard (ISTD). The method gives excellent sensitivity for all the alkyl and aryl esters at typical target analyte level, according to the acceptance criteria that are described in the Guideline on the Limits of Genotoxic Impurities which has been issued in 2007 by the European Medicines Agency (EMA). The average recovery for methanesulfonic ac... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5478657 Thu, 17 Nov 2011 05:00:00 +0100 5478657 http://www.medworm.com/index.php?rid=5478656&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22115866%26dopt%3DAbstract Authors: Telbisz A, Hegedüs C, Ozvegy-Laczka C, Goda K, Várady G, Takáts Z, Szabó E, Sorrentino BP, Váradi A, Sarkadi B Abstract The ABCG2 multidrug transporter protein has been identified as a key player in cancer drug resistance and xenobiotic elimination, as its actively transported substrates include anticancer drugs, intermediates of heme metabolism, xenobiotics, and also drug conjugates. Several transported substrates at higher concentrations, and some anticancer agents even at low concentrations directly inhibit the ABCG2 transporter, thus it is difficult to provide estimation for pharmacologically important ABCG2-dependent interactions. In addition, as documented here, in mutant variants of the transporter, inhibitors of the wild-type ABCG2 may become actively transpor... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5478656 Thu, 17 Nov 2011 05:00:00 +0100 5478656 http://www.medworm.com/index.php?rid=5478655&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22115867%26dopt%3DAbstract Authors: Wilczyński S, Pilawa B, Koprowski R, Wróbel Z, Ptaszkiewicz M, Swakoń J, Olko P Abstract Radiation sterilization technology is more actively used now that any time because of its many advantages. Gamma radiation has high penetrating power, relatively low chemical reactivity and causes small temperature rise. But on the other hand radiosterilization can lead to radiolytic products appearing, in example free radicals. Free radicals in radiative sterilized sisomicin, tobramycin and paromomycin were studied by electron paramagnetic resonance (EPR) spectroscopy. Dose of gamma irradiation of 25kGy was used. Concentrations and properties of free radicals in irradiated antibiotics were studied. EPR spectra were recorded for samples stored in air and argon. For gamma irradiated ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5478655 Thu, 17 Nov 2011 05:00:00 +0100 5478655 http://www.medworm.com/index.php?rid=5478654&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22115868%26dopt%3DAbstract Authors: Kitamura K, Niinobu M, Omran AA, Takegami S, Kitade T Abstract Simultaneous specific and nonspecific binding of bendroflumethiazide (BFZ) to human serum albumin (HSA) and concentration profile of BFZ in HSA buffer (pH 7.40) solution were investigated by (19)F nuclear magnetic resonance (NMR) method. The (19)F NMR spectrum of BFZ (200μM) in a buffer solution showed a sharp signal of its CF(3) group at 17.8ppm from the reference trifluoroethanol. Addition of 0.60mM HSA to the sample solution caused the CF(3) signal splitting into three broadened peaks at 18.4 (A), 17.9 (B) and 17.4ppm (C). By its chemical shift and spectral behavior, B was assigned to unbound BFZ. Competition experiments with Site I and II ligands lead to C being assigned to Site II bound BFZ. However, the ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5478654 Thu, 17 Nov 2011 05:00:00 +0100 5478654 http://www.medworm.com/index.php?rid=5446294&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22108344%26dopt%3DAbstract Authors: Di Pretoro G, Zema L, Palugan L, Wilson DI, Rough SL, Gazzaniga A Abstract Pellets with high loading of 5-aminosalicylic acid (5-ASA, mesalamine) are desired to reduce the number of tablets required to deliver the daily dosing regimen. Recently, we reported an extrusion-spheronisation route for the development of a 90wt% 5-ASA/microcrystalline cellulose formulation based on milled 5-ASA which gave good yields of pellets at the lab scale. In the present work, such formulation was optimised further by preliminary studies using a lab-scale ram extruder, and then scaled up to the pilot plant scale on a Nica screen extruder using a mixed fractional factorial approach. The final formulation featured 95wt% 5-ASA and 5wt% Avicel RC591 (all dry basis) and yielded spherical pellets ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5446294 Wed, 16 Nov 2011 05:00:00 +0100 5446294 http://www.medworm.com/index.php?rid=5446292&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22108346%26dopt%3DAbstract Authors: Karlsson D, Fallarero A, Brunhofer G, Guzik P, Prinz M, Holzgrabe U, Erker T, Vuorela P Abstract In this contribution, a chemical collection of aromatic compounds was screened for inhibition on butyrylcholinesterase (BChE)'s hydrolase activity using Ellman's reaction. A set of diarylimidazoles was identified as highly selective inhibitors of BChE hydrolase activity and amyloid β (Aβ) fibril formation. New derivatives were synthesized resulting in several additional hits, from which the most active was 6c, 4-(3-ethylthiophenyl)-2-(3-thienyl)-1H-imidazole, an uncompetitive inhibitor of BChE hydrolase activity (IC(50) BChE=0.10μM; K(i)=0.073±0.011μM) acting also on Aβ fibril formation (IC(50)=5.8μM). With the aid of structure-activity relationship (SAR) studies, chemic... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5446292 Wed, 16 Nov 2011 05:00:00 +0100 5446292 http://www.medworm.com/index.php?rid=5446290&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22108348%26dopt%3DAbstract Authors: Mühlfeld L, Langguth P, Häusler H, Hagels H Abstract A sealability of aluminium lidding foils against formable polymer materials of blister packages is usually achieved by a coating of aluminium with certain grammages of heat seal lacquers. To investigate influences of their thickness on quality of blister packages, lidding foils with different grammages of two lacquer types were manufactured. Sealing experiments (variation of temperature, pressure and sealing time) were performed. Sealed seam strengths were determined with mechanical tensile tests, tightness of cold form blisters were analysed by means of helium leakage tests. Time-dependent moisture uptake of stored blisters was monitored with micro-gas chromatography. By means of a simple calculation model the permeab... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5446290 Wed, 16 Nov 2011 05:00:00 +0100 5446290 http://www.medworm.com/index.php?rid=5446293&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22108345%26dopt%3DAbstract Authors: Onoue S, Matsui T, Aoki Y, Ishida H, Nukaya H, Kou K, Yamada S Abstract Chafuroside A (CFA), a poorly water-soluble flavone C-glycoside, was firstly isolated from oolong tea, and it acts as a potent anti-inflammatory agent. The present study was undertaken to develop a water-soluble formulation of CFA using a self-assembled micellar (SAM) system, with the aim of improved dissolution behavior and potent anti-inflammatory effects. The SAM formulation of CFA (CFA/SAM) was characterized in terms of its morphology, particle size distribution, crystallinity, and dissolution behavior. In dissolution testing, the CFA/SAM exhibited marked improvement in dissolution behavior when compared with crystalline CFA, and then, nano-micellar particles were constituted with a mean diameter o... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5446293 Sun, 13 Nov 2011 05:00:00 +0100 5446293 http://www.medworm.com/index.php?rid=5446291&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22108347%26dopt%3DAbstract CONCLUSION: UA can reduce the over expression of CRP in HepG2 cells induced by IL-6 and inhibit the increased expression of VCAM-1 and LOX-1 in HUVECs caused by CRP. Our research suggests that UA can reduce CRP levels in plasma and prevent inflammatory cytokines from injuring endothelial cells by inhibiting the hepatic synthesis of CRP. So UA may have positive significance for prevention and treatment of atherosclerosis and other cardiovascular diseases. PMID: 22108347 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5446291 Sun, 13 Nov 2011 05:00:00 +0100 5446291 http://www.medworm.com/index.php?rid=5446295&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22101136%26dopt%3DAbstract In this study several Machine Learning methods, including the K-nearest-neighbour (KNN) regression, single layer networks, radial basis function networks and the SVM classifier were applied to an enhancer dataset reported previously. The SMOTE sampling method was used to oversample chemical compounds with ER>10 in each training set in order to improve estimation of GP and KNN. Results show that models using five physicochemical descriptors exhibit better performance than those with three features. The best classification result was obtained by using the SVM method without dealing with imbalanced data. Following over-sampling, GP gives the best result. It correctly assigned 8 of the 12 "good" (ER>10) enhancers and 56 of the 59 "poor" enhancers (ER<10). Overall success rates were si... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5446295 Fri, 11 Nov 2011 05:00:00 +0100 5446295 http://www.medworm.com/index.php?rid=5427795&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085633%26dopt%3DAbstract Authors: Storm G PMID: 22085633 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427795 Thu, 10 Nov 2011 05:00:00 +0100 5427795 http://www.medworm.com/index.php?rid=5427787&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22094306%26dopt%3DAbstract Authors: Croes S, Koop AH, van Gils SA, Neef C Abstract Therapeutic drug monitoring (TDM) of aminoglycosides has been a topic during the last thirty years. There is a tendency that - because of the once-daily regimen - TDM is considered not necessary anymore. Although once daily dosing has the potential for decreased toxicity, long-term usage can cause severe nephro- and ototoxicity. Furthermore, inadequate plasma concentrations can lead to treatment failure. This work is devoted to the development and application of the first mathematical model of aminoglycosides, which simulates in relation to the pharmacokinetics both their effects on bacteria as well as their nephrotoxicity and cochleotoxicity. Our software system is suitable for TDM. Based on theoretical considerations, a mult... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427787 Thu, 10 Nov 2011 05:00:00 +0100 5427787 http://www.medworm.com/index.php?rid=5427796&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085632%26dopt%3DAbstract In this study, the glucosamine-based polymer chitosan was used as a cationic polymer-based in vitro delivery system for GLP-1, DPP-IV resistant GLP-1 analogues and siRNA targeting DPP-IV mRNA. We found chitosans to form spherical nanocomplexes with these nucleic acids, generating two distinct non-overlapping size ranges of 141-283nm and 68-129nm for plasmid and siRNA, respectively. The low molecular weight high DDA chitosan 92-10-5 (degree of deacetylation, molecular weight and N:P ratio (DDA-Mn-N:P)) showed the highest plasmid DNA transfection efficiency in HepG2 and Caco-2 cell lines when compared to 80-10-10 and 80-80-5 chitosans. Recombinant native GLP-1 protein levels in media of transfected cells reached 23ng/L while our DPP-IV resistant analogues resulted in a fivefold increase of G... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427796 Wed, 09 Nov 2011 05:00:00 +0100 5427796 http://www.medworm.com/index.php?rid=5427794&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085634%26dopt%3DAbstract Authors: Haug KG, Weber B, Hochhaus G, Butterweck V Abstract Ammi visnaga L. (syn. Khella, Apiaceae) preparations have traditionally been used in the Middle East for the treatment of kidney stone disease. Visnagin, a furanocoumarin derivative, is one of the main compounds of Ammi visnaga with potential effects on kidney stone prevention. To date, no information is available about the pharmacokinetic (PK) properties of visnagin. It was the aim of the study to characterize the PK properties of visnagin after intravenous (i.v.) bolus administration in rats and to develop an adequate model for the description of the observed data, including model parameter estimates. Therefore, three doses of visnagin (1.25, 2.5, and 5mg/kg) solubilized in 25% Captisol® were administered by i.v. bolus... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427794 Wed, 09 Nov 2011 05:00:00 +0100 5427794 http://www.medworm.com/index.php?rid=5427793&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085635%26dopt%3DAbstract Authors: Zhong Y, Dai Z, Xu Y, Teng Y, Wu B Abstract A novel codrug (LMX) was obtained from lamivudine (LMV) and ursolic acid (UA) coupled with ethyl chloroacetate through an amide and ester linkage. The structure of LMX was confirmed by (1)H NMR, (13)C NMR, IR and HRMS. Herein, the in vitro non-enzymatic and enzymatic hydrolysis and in vivo pharmacological activities of LMX were studied. The kinetics of hydrolysis of LMX was studied in aqueous solution of pH 1-10, 80% buffered human plasma and in the presence of lipase from Porcine pancreas (EC 3.1.1.3) at 37°C. It is found that LMX hydrolysis rate was significantly faster in lipase with half-life of 1.4h compared to pH 7.4 phosphate buffer (t(1/2) 11.2h) and buffered human plasma (t(1/2) 5.4h). The decomposition rates in aqueous... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427793 Wed, 09 Nov 2011 05:00:00 +0100 5427793 http://www.medworm.com/index.php?rid=5427792&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085636%26dopt%3DAbstract Authors: Lebedeva G, Sorokin A, Faratian D, Mullen P, Goltsov A, Langdon SP, Harrison DJ, Goryanin I Abstract High levels of variability in cancer-related cellular signalling networks and a lack of parameter identifiability in large-scale network models hamper translation of the results of modelling studies into the process of anti-cancer drug development. Recently global sensitivity analysis (GSA) has been recognised as a useful technique, capable of addressing the uncertainty of the model parameters and generating valid predictions on parametric sensitivities. Here we propose a novel implementation of model-based GSA specially designed to explore how multi-parametric network perturbations affect signal propagation through cancer-related networks. We use area-under-the-curve for t... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427792 Wed, 09 Nov 2011 05:00:00 +0100 5427792 http://www.medworm.com/index.php?rid=5427791&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085679%26dopt%3DAbstract Authors: Tran VT, Karam JP, Garric X, Coudane J, Benoît JP, Montero-Menei CN, Venier-Julienne MC Abstract A promising strategy to repair injured organs is possible by delivering a growth factor via poly-(d,l lactide-co-glycolide) (PLGA) microspheres; the latter are coated with adhesion molecules that serve as a support for cell delivery. At present, PLGA is not the optimal choice of polymer because of poor or incomplete protein release. The use of a more hydrophilic PLGA-PEG-PLGA (A-B-A) copolymer increases the degree of protein release. In this work, the impact of different combinations of (B) and (A) segments on the protein-release profile has been investigated. Continuous-release profiles, with no lag phases, were observed. The triblock ABA with a low molecular weight of PEG an... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427791 Wed, 09 Nov 2011 05:00:00 +0100 5427791 http://www.medworm.com/index.php?rid=5427790&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085680%26dopt%3DAbstract Authors: Ma Y, Gao H, Gu W, Yang YW, Wang Y, Fan Y, Wu G, Ma J Abstract Poly(glycerol methacrylate)s (PGOHMAs) were successfully synthesized via the hydrolysis of the epoxy groups on linear and/or star-shaped poly(glycidyl methacrylate)s (PGMAs). Further modification of the hydroxyl groups on PGOHMAs with succinic anhydride (SA) or 1,2-cyclohexanedicarboxylic anhydride (CDA) resulted in a new type of polyacid polymer, namely, PGOHMACOOH for short, which was then employed to prepare pH-sensitive assemblies using dialysis method. The carboxylated polymers were quite effective in the encapsulation of doxorubicin hydrochloride (DOX) by electrostatic interaction. Compared with poly(acrylic acid) (PAA), the star-shaped PGOHMA modified with CDA exhibited higher encapsulation efficiency an... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427790 Wed, 09 Nov 2011 05:00:00 +0100 5427790 http://www.medworm.com/index.php?rid=5427789&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085681%26dopt%3DAbstract Authors: Ikarashi N, Mimura A, Kon R, Iizasa T, Omodaka M, Nagoya C, Ishii M, Toda T, Ochiai W, Sugiyama K Abstract Patients with severe constipation are treated with combinations of several different laxatives. The purpose of this study is to examine whether the concomitant use of different laxatives enhances the laxative effect, using an osmotic laxative, magnesium sulphate (MgSO(4)), and a stimulant laxative, bisacodyl. The faecal water content of rats, to which MgSO(4) and bisacodyl were coadministered, was lower than that in the MgSO(4) group, while the change in the faecal water content over time was very similar to that in the bisacodyl group. The mRNA expression of the osmotic pressure marker, sodium/myo-inositol transporter, in the coadministration group 5h after the admin... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427789 Wed, 09 Nov 2011 05:00:00 +0100 5427789 http://www.medworm.com/index.php?rid=5427788&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085682%26dopt%3DAbstract The objectives of this study were to determine the effects of Tricin 7-glucoside on a cultured neuronal cell line, SH-SY5Y in vitro and experimental ischemic stroke in vivo. For oxygen-glucose deprivation (OGD) and tumor necrosis factor-α (TNF-α) stimulated SH-SY5Y cell line in vitro, SH-SY5Y cells were incubated with Tricin 7-glucoside. For in vivo experiment, rats were subjected to middle cerebral artery occlusion (MACO) for 1h, then followed by reperfusion for 23h. Treatment of SH-SY5Y cells with Tricin 7-glucoside reduced the OGD-induced apoptosis and cytotoxicity, blocked TNF-α-induced NF-κB and IκB-α phosphorylation, and decreased HMGB1 expression. At doses higher than 50mg/kg, Tricin 7-glucoside produced a significant neuroprotective potential in rats with ischemia and reperfu... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427788 Mon, 07 Nov 2011 05:00:00 +0100 5427788 http://www.medworm.com/index.php?rid=5427798&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22079137%26dopt%3DAbstract Authors: Soares DC, Cardoso VN, de Barros AL, de Souza CM, Cassali GD, de Oliveira MC, Ramaldes GA Abstract In the present study, PEG-coated pH-sensitive and PEG-folate-coated pH-sensitive liposomes containing the (159)Gd-DTPA-BMA were prepared and radiolabeled through neutron activation technique, aiming to study the in vivo antitumoral activity and toxicity on mice bearing a previously-developed solid Ehrlich tumor. The treatment efficacy was verified through tumoral volume increase and histomorphometry studies. The toxicity of formulations was investigated through animal weight variations, as well as hematological and biochemical tests. The results showed that after 31days of treatment, animals treated with radioactive formulations had a lower increase in tumor volume and a sign... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427798 Fri, 04 Nov 2011 04:00:00 +0100 5427798 http://www.medworm.com/index.php?rid=5427797&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22079138%26dopt%3DAbstract Authors: Cai H, Ni C, Zhang L Abstract Monodispersed complex nano-particles were synthesized simply by mixing alginic acid (ALG-H) with poly[(2-dimethylamino) ethyl methacrylate] (PDEMA) in pure water without any surfactants or additives. The structure and properties of the nano-particles were extensively studied. The surface charges and average sizes of the nano-particles were varied with the composition of ALG-H and PDEMA. The nano-particles were formed through electrostatic attraction force, and they were very stable in pure water, but dissociated in salt solutions. An anticancer drug (doxorubicin) was loaded in the nano-particles and released in different saline solutions. The release profiles revealed that the drug release could be controlled by adjusting the pH and salt conce... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427797 Fri, 04 Nov 2011 04:00:00 +0100 5427797 http://www.medworm.com/index.php?rid=5427800&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22067974%26dopt%3DAbstract Authors: Vadia N, Rajput S Abstract The aim of this study was to develop methotrexate loaded mesoporous MCM-41 nanoparticles for improved dissolution of methotrexate. The mesoporous MCM-41 nanoparticles act as carrier for drug and increase the solubility of the drug. In order to achieve this objective small pore size MCM-41 nanoparticles have been synthesized followed by drug loading process. The process of drug loading was optimized using full 3(3) factorial design. With a view to obtain maximum drug loading three variables, concentration of drug solution, stirring rate, and drug:carrier ratio were optimized using a full 3(3) factorial design. Using statistically designed experiments, the inclusion of methotrexate in MCM-41 nanoparticles was successfully carried out to obtain a dr... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427800 Mon, 31 Oct 2011 04:00:00 +0100 5427800 http://www.medworm.com/index.php?rid=5427799&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22074938%26dopt%3DAbstract This study has also revealed that CL spectroscopy can distinguish between crystalline and amorphous materials and is sensitive the differences between the solid forms of some organic compounds, such as salts and polymorphs. Up to 80% of commonly used excipients are non-cathodoluminescent and this has the advantage of enabling APIs in formulated products to be imaged without interference. As part of the investigation to explore the use of CL as a way to identify polymorphs and monitor phase transformations, it was discovered that by recrystallising fused carbamazepine, the metastable Form IV was unexpectedly produced. PMID: 22074938 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427799 Mon, 31 Oct 2011 04:00:00 +0100 5427799 http://www.medworm.com/index.php?rid=5427804&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22064451%26dopt%3DAbstract Authors: Wang T, Zou M, Jiang H, Ji Z, Gao P, Cheng G Abstract The purpose of this study is to develop a novel kind of adjuvant for oral vaccine delivery. In order to effectively prevent the degradation of antigens in the gastrointestinal tract and optimize the uptake for M cells, a novel kind of hydrophobic carbon nanoparticle (C1) with the size of 470nm was synthesized by taking silica as a template and sucrose as a carbon source. Notably, there were large mesopores and macropores mainly of 40-60nm, which made it to be excellent candidate as an antigen carrier. C1 was characterized using SEM, TEM and nitrogen adsorption. Following oral immunization with BSA loaded in C1, the IgG titer reached to a level almost equal to that of parenteral administration of antigen emulsified in Fr... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427804 Fri, 28 Oct 2011 04:00:00 +0100 5427804 http://www.medworm.com/index.php?rid=5427803&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22064452%26dopt%3DAbstract Authors: Tiwari MD, Mehra S, Jadhav S, Bellare JR Abstract All-trans retinoic acid (atRA) is used in the differentiation therapy of Acute Promyelocytic Leukemia. However, its therapeutic success is limited by the appearance of relapse and recalcitrant cases, poor aqueous solubility and high degradability. In the current work, we prepared two types of atRA-loaded copolymer nanoparticles - PL1RA and PC1RA, based on poly(ethyleneglycol) (PEG)-poly(l-lactide) and PEG-poly(ε-caprolactone), respectively. We then evaluated their physico-chemical properties and compared their differentiation-inducing potential of HL-60 cells with free atRA. These nanoparticles were in the size range 100-150nm, possessed moderate colloidal stability and exhibited around 30% encapsulation efficiencies. In v... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427803 Fri, 28 Oct 2011 04:00:00 +0100 5427803 http://www.medworm.com/index.php?rid=5427802&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22064453%26dopt%3DAbstract In this study, we examined the in vitro insulin dissolution behavior and the in vivo pharmacokinetics and pharmacodynamics after subcutaneous administration of PM-insulin sol (PM-Isol). In the in vitro release study, after PM-Isol was converted to a gel phase (PM-Igel), PM concentration-dependent and controlled release of insulin were observed at the final concentrations of PM between 0.1% and 2.0% (w/v). The PM-Isol is changed to gel form in vivo, and exhibited a sustained-release pharmacokinetics of insulin, where PM concentration-dependent prolongation of efficacy was found. The plasma glucose level markedly decreased, and the lowest plasma glucose level was maintained up to 24h when 2.0% (w/v) PM-Isol was administered subcutaneously to rats. The PM-Isol, we developed here, is applicabl... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427802 Fri, 28 Oct 2011 04:00:00 +0100 5427802 http://www.medworm.com/index.php?rid=5427801&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22064454%26dopt%3DAbstract Authors: Altintas I, Kok RJ, Schiffelers RM Abstract The discovery of naturally occurring heavy chain only antibodies and their further development into small recombinant 'nanobodies' offers attractive applications in drug targeting. Here, we describe the properties of nanobodies that have been developed to target the epidermal growth factor receptor (EGFR) and contrast these to the characteristics of heavy chain only antibodies and conventional antibodies. EGFR is overexpressed in many tumors and is an attractive target for tumor-directed drug targeting. PMID: 22064454 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5427801 Fri, 28 Oct 2011 04:00:00 +0100 5427801 http://www.medworm.com/index.php?rid=5363461&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22033153%26dopt%3DAbstract Authors: Lakshmanan AP, Thandavarayan RA, Palaniyandi SS, Sari FR, Meilei H, Giridharan VV, Soetikno V, Suzuki K, Kodama M, Watanabe K Abstract There is evidence that the activation of renal angiotensin (Ang)-II plays a critical role in the pathogenesis of diabetic kidney diseases (DN) via the ER stress-induced renal apoptosis. Since, the potential negative role of Ang-II in the pathogenesis of ER stress-mediated apoptosis is poorly understood; we evaluated whether treatment of mice with AT-1R specific blocker, olmesartan is associated with the reduction of ER stress induced renal apoptosis in streptozotocin (STZ)-induced diabetic animal model. We employed western blot analysis to measure the renal protein expressions level of NADPH oxidase subunits, ER chaperone GRP78 and an ER-as... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363461 Thu, 20 Oct 2011 04:00:00 +0100 5363461 http://www.medworm.com/index.php?rid=5363462&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22033152%26dopt%3DAbstract In this study, photometric stereo imaging was applied in real-time during the final steps of the ES process, being spheronization and drying. In addition to the pellet size distribution of undispersed (wet) samples, the imaging technique captures visual information on pellet shape and surface brightness. Pellet samples were taken at 20 time points during spheronization and were imaged at-line (during spheronization) and off-line (after spheronization). Particle size distributions and visual image information were both used to characterise the spheronization behaviour of different formulations. Next, particle size distributions and surface brightness values calculated from the at-line obtained images during fluid bed drying of pellets were analysed. The particle size distribution and bright... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363462 Wed, 19 Oct 2011 04:00:00 +0100 5363462 http://www.medworm.com/index.php?rid=5363464&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22024381%26dopt%3DAbstract Authors: Wu JX, Yang M, Berg FV, Pajander J, Rades T, Rantanen J Abstract New chemical entities (NCEs) often show poor water solubility necessitating solid dispersion formulation. The aim of the current study is to employ design of experiments in investigating the influence of one critical process factor (solvent evaporation rate) and two formulation factors (PVP:piroxicam ratio (PVP:PRX) and PVP molecular weight (P(MW))) on the physical stability of PRX solid dispersion prepared by the solvent evaporation method. The results showed the rank order of an increase in factors contributing to a decrease in the extent of PRX nucleation being evaporation rate>PVP:PRX>P(MW). The same rank order was found for the decrease in the extent of PRX crystal growth in PVP matrices from day 0... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363464 Mon, 17 Oct 2011 04:00:00 +0100 5363464 http://www.medworm.com/index.php?rid=5363463&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22024382%26dopt%3DAbstract Authors: Vellema J, Hunfeld NG, Van den Akker HE, Ter Horst JH Abstract Lorazepam is a strong sedative for intensive care patients and a commonly used method of administering it to the patient is by infusion of a freshly prepared lorazepam solution. During lorazepam infusion often unwanted lorazepam crystallization occurs, resulting in line obstruction and reduced lorazepam concentrations. With the aid of solubility measurements a solid-liquid phase diagram for lorazepam in mixtures of a commercially available lorazepam solution and an aqueous glucose solution was determined. This confirmed that the glucose solution acts as an anti-solvent, greatly reducing the lorazepam solubility in the infusion solution. Three approaches are proposed to obtain stable lorazepam solutions upon mix... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363463 Mon, 17 Oct 2011 04:00:00 +0100 5363463 http://www.medworm.com/index.php?rid=5363467&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22019492%26dopt%3DAbstract We examined and compared the effect of exogenous LPC on intracellular Ca(2+) overload in human Jurkat CD4+ T lymphocytes and mouse CTLL-2 CD8+ T lymphocytes. LPC caused a dose-dependent intracellular Ca(2+) level ([Ca(2+)](i)) increase in both Jurkat and CTLL-2 lymphocytes. Pretreatment of cells for 5min with 30μM of ruthenium red, a potent ryanodine receptor inhibitor, reduced the LPC-induced Ca(2+) response in both Jurkat and CTLL-2 T lymphocytes. Moreover, pretreatment of cells with 100μM 2-APB for 15min, a cell-permanent IP(3) receptor inhibitor, reduced about two thirds of the LPC induced calcium response in both kinds of cells. However, preincubation of the cells with verapamil, an L-type Ca(2+) channel blocker, did not affect the LPC-induced [Ca(2+)](i) increase in CTLL-2 lymphocy... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363467 Fri, 14 Oct 2011 04:00:00 +0100 5363467 http://www.medworm.com/index.php?rid=5363466&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22019523%26dopt%3DAbstract Authors: Ménard N, Tsapis N, Poirier C, Arnauld T, Moine L, Lefoulon F, Péan JM, Fattal E Abstract To overcome poor water-solubility of new drug candidates, four innovative surfactants based on naturally-occuring hydrophilic and hydrophobic moities were designed and synthesized: cholesteryl-glutamic acid, cholesteryl-poly[N-2-hydroxyethyl-l-glutamine] (PHEG), ursodeoxycholanyl-PHEG (UDCA-PHEG) and ursodeoxycholanyl-poly-l-glutamic acid (UDCA-PGA). Their self-assembling capacity was evaluated using pyrene fluorescence measurements which allow to determine their critical aggregation concentration (CAC). Size measurements were carried out using dynamic light scattering (DLS). Surfactant cytotoxicity was investigated on human umbilical vein endothelial cells (HUVEC) by determining te... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363466 Thu, 13 Oct 2011 04:00:00 +0100 5363466 http://www.medworm.com/index.php?rid=5363465&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22019524%26dopt%3DAbstract In conclusion, the current study demonstrated that matrine exhibited a protective effect on LPS-induced acute lung injury by inhibiting of the inflammatory response, which may involve the suppression of ROS and tissue oxidative stress. PMID: 22019524 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363465 Thu, 13 Oct 2011 04:00:00 +0100 5363465 http://www.medworm.com/index.php?rid=5363472&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22009109%26dopt%3DAbstract Authors: Luppi B, Bigucci F, Corace G, Delucca A, Cerchiara T, Sorrenti M, Catenacci L, Di Pietra AM, Zecchi V Abstract Peroral administration of tacrine, the first acetylcholinestearse inhibitor licensed for the treatment of Alzheimer's disease, is associated with low bioavailability, due to an extended first-pass methabolism, short elimination half-life and hepatotoxicity. Nasal drug delivery may reduce the degree of these problems. Tacrine hydrochloride nasal delivery is here investigated by means of albumin nanoparticles carrying beta cyclodextrin and two different beta cyclodextrin derivatives (hydroxypropyl beta cyclodextrin and sulphobutylether beta cyclodextrin). Bovine serum albumin nanoparticles were obtained using a coacervation method, followed by thermal cross-linking,... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363472 Sat, 08 Oct 2011 04:00:00 +0100 5363472 http://www.medworm.com/index.php?rid=5363471&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22009110%26dopt%3DAbstract Authors: Vaidya B, Agrawal GP, Vyas SP Abstract The present study was aimed to study the effect of RGD peptide conjugation on the bio-distribution behaviour of long circulatory liposomes in the thrombosed rat model. Further, thrombolysis study was also performed to evaluate the therapeutic activity of the prepared liposomes. Liposomes were prepared by film hydration method and peptide was subsequently conjugated on the preformed liposomes using carbodiimide chemistry. Prepared liposomes were characterized for size and size distribution, entrapment efficiency and in vitro drug release. In vitro targeting ability of the liposomes was determined by platelets binding assay. In vivo studies were performed in the rat model containing human blood clot inoculated in the carotid artery. Res... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363471 Sat, 08 Oct 2011 04:00:00 +0100 5363471 http://www.medworm.com/index.php?rid=5363470&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22009111%26dopt%3DAbstract In conclusion, the biodegradable LTB(4)/CFAgs-loaded MS were able to efficiently activate murine BMDMϕ and thereby have the potential to be used in an effective vaccine against H. capsulatum infection. PMID: 22009111 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363470 Sat, 08 Oct 2011 04:00:00 +0100 5363470 http://www.medworm.com/index.php?rid=5363469&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22009112%26dopt%3DAbstract Authors: Verheul RJ, Hagenaars N, van Es T, van Gaal EV, de Jong PH, Bruijns S, Mastrobattista E, Slütter B, Que I, Heldens JG, van den Bosch H, Glansbeek HL, Hennink WE, Jiskoot W Abstract Recently we reported that reacetylation of N,N,N-trimethyl chitosan (TMC) reduced the adjuvant effect of TMC in mice after intranasal (i.n.) administration of whole inactivated influenza virus (WIV) vaccine. The aim of the present study was to elucidate the mechanism of this lack of adjuvanticity. Reacetylated TMC (TMC-RA, degree of acetylation 54%) was compared with TMC (degree of acetylation 17%) at six potentially critical steps in the induction of an immune response after i.n. administration in mice. TMC-RA was degraded in a nasal wash to a slightly larger extent than TMC. The local i.n. di... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363469 Sat, 08 Oct 2011 04:00:00 +0100 5363469 http://www.medworm.com/index.php?rid=5363468&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22009113%26dopt%3DAbstract Authors: Bal SM, Slütter B, Verheul R, Bouwstra JA, Jiskoot W Abstract N-trimethyl chitosan (TMC) nanoparticles have been shown to increase the immunogenicity of subunit antigens after nasal and intradermal administration. This work describes a second generation of TMC nanoparticles containing ovalbumin as a model antigen (TMC/OVA nanoparticles) and an immunopotentiator (TMC/OVA/immunopotentiator nanoparticles). The selection of immunopotentiators included Toll-like receptor (TLR) ligands lipopolysaccharide (LPS), PAM(3)CSK(4) (PAM), CpG DNA, the NOD-like receptor 2 ligand muramyl dipeptide (MDP) and the GM1 ganglioside receptor ligand, cholera toxin B subunit (CTB). The TMC/OVA/immunopotentiator nanoparticles were characterised physico-chemically and their immunogenicity was asse... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363468 Sat, 08 Oct 2011 04:00:00 +0100 5363468 http://www.medworm.com/index.php?rid=5363473&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22001125%26dopt%3DAbstract Authors: Isacchi B, Fabbri V, Galeotti N, Bergonzi MC, Karioti A, Ghelardini C, Vannucchi MG, Bilia AR Abstract Salvianolic acid B (SalB) represents the most characteristic constituent of Salvia miltiorrhiza Bge. with a strong free radicals scavenger activity. This property may be useful in the treatment of some severe chronic diseases, where there is an imbalance of reactive oxygen species formation and where intracellular reactive oxygen and nitrogen species level can cause severe cell damage and even cell death. In particular, SalB can protect against the oxidative stress as well as the antioxidant superoxide dismutase and reduced activity of glutathione, important determinants of neuropathological and behavioural consequences in neuropathic pain. This is a chronic disease defin... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5363473 Tue, 04 Oct 2011 04:00:00 +0100 5363473 http://www.medworm.com/index.php?rid=5316795&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21986445%26dopt%3DAbstract Authors: Cadete A, Figueiredo L, Lopes R, Calado CC, Almeida AJ, Gonçalves LM Abstract Chitosan is one of the most promising polymers for drug delivery through the mucosal routes because of its polycationic, biocompatible, and biodegradable nature, and particularly due to its mucoadhesive and permeation-enhancing properties. Bile salts are known to interact with lipid membranes, increasing their permeability. The addition of bile salts to chitosan matrices may improve the delivery characteristics of the system, making it suitable for mucosal administration of bioactive substances. In the present study we have developed chitosan nanoparticles using sodium deoxycholate as a counter ion and evaluated their potential as gene delivery carriers. Chitosan-sodium deoxycholate nanoparticle... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5316795 Sat, 01 Oct 2011 04:00:00 +0100 5316795 http://www.medworm.com/index.php?rid=5316796&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21983568%26dopt%3DAbstract Authors: Lopes R, Eleutério CV, Gonçalves LM, Cruz ME, Almeida AJ Abstract Oryzalin is a dinitroaniline drug that has attracted recent interest for the treatment of leishmaniasis. Its use as an antiparasitic therapeutic agent is limited by the low water solubility associated with an in vivo rapid clearance, leading to the administration of larger and possibly toxic doses in in vivo studies, and the use of solvents that may lead to undesirable side effects. In the present work oryzalin-containing lipid nanoparticles were produced by a emulsion-solvent evaporation technique using a composition suitable for parenteral administration, i.e., tripalmitin (solid lipid) and a complex mixture of three emulsifying agents (soya lecithin, Tween® 20 and sodium deoxycholate). Physicochemical ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5316796 Thu, 29 Sep 2011 04:00:00 +0100 5316796 http://www.medworm.com/index.php?rid=5284005&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21968337%26dopt%3DAbstract Authors: Stegemann S, Klebovich I, Antal I, Blume HH, Magyar K, Németh G, Paál TL, Stumptner W, Thaler G, Van de Putte A, Shah VP Abstract With a New Drug Application (NDA) innovative drug therapies are reaching the market in a specific dosage form for one or more clinically proven indications of which after expiration of the patent or the data exclusivity copies are launched using Abbreviated New Drug Applications (ANDA). Advanced therapies that emerged from launched molecules during their product life-cycle have gained considerable attention as clinical practice provides evidence for additional therapeutic values, patient centric delivery systems show improved therapeutic outcomes or emerging technologies offer efficiency gains in manufacturing or access to emerging markets. Th... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284005 Sat, 24 Sep 2011 04:00:00 +0100 5284005 http://www.medworm.com/index.php?rid=5284010&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963456%26dopt%3DAbstract Authors: Kataoka M, Yokoyama T, Masaoka Y, Sakuma S, Yamashita S Abstract The purpose of this study was to establish an in vitro system that evaluates the effects of P-glycoprotein (P-gp)-mediated efflux on the oral absorption of P-gp substrates. An in vitro system (dissolution/permeation system, D/P system) was developed that consisted of apical and basal chambers and a Caco-2 cell monolayer mounted between the chambers. Both sides of the monolayer were filled with physiological solution and were stirred at 200rpm. The dissolution in the apical medium and permeation to the basal medium were monitored for 2h after P-gp substrates were applied to the apical side of the system. When erythromycin existed in the apical medium, the permeations of fexofenadine and talinolol were signific... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284010 Thu, 22 Sep 2011 04:00:00 +0100 5284010 http://www.medworm.com/index.php?rid=5284009&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963457%26dopt%3DAbstract Authors: Zsóka W, Judit C, Csaba R, László R, János S, Zoltán R Abstract Immunosafety analysis of pharmaceutical surfactants is an important step in understanding the complex mechanisms by which they induce side effects in susceptible patients. This paper provides experimental evidences that polyethoxylated surfactants, Cremophor-EL and Tween-80, also known as Polysorbate-80, activate the complement system in vitro, in normal human serum and plasma. They appeared to be more efficient reactogens than their structural homolog, Tween-20. Cremophor-EL and Tween-80 promoted the generation of biologically active complement products, C3a, C5a and C5b-9. Consistently, Paclitaxel and Taxotere (Docetaxel), pharmaceuticals formulated in Cremophor-EL and Tween-80, activated the complement... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284009 Thu, 22 Sep 2011 04:00:00 +0100 5284009 http://www.medworm.com/index.php?rid=5284007&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21964204%26dopt%3DAbstract Authors: Katiyar D, Singh B, Lall AM, Haldar C Abstract The present study evaluates the effects of chitooligosaccharides (COS) for the management of alloxan induced diabetes in mice. For the management of the carbohydrate metabolism in diabetes by the COS, the amount of glucose in blood along with quantification of glycogen in liver were measured and noted a significant recovery in respect to diabetic control group. As hyperlipidemia and oxidative stress are the disorders of diabetes so, we have also assessed the serum levels of total cholesterol (TC), triglyceride (TG), low density lipoprotein cholesterol (LDLc), very low density lipoprotein cholesterol (VLDLc) and high density lipoprotein cholesterol (HDLc). For the recovery of oxidative stress the SOD MDA catalase in liver and G... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284007 Thu, 22 Sep 2011 04:00:00 +0100 5284007 http://www.medworm.com/index.php?rid=5284008&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21964203%26dopt%3DAbstract Authors: El-Gendy N, Pornputtapitak W, Berkland C Abstract Particle engineering strategies remain at the forefront of aerosol research for localized treatment of lung diseases and represent an alternative for systemic drug therapy. With the hastily growing popularity and complexity of inhalation therapy, there is a rising demand for tailor-made inhalable drug particles capable of affording the most proficient delivery to the lungs and the most advantageous therapeutic outcomes. To address this formulation demand, nanoparticle agglomeration was used to develop aerosols of the asthma therapeutics, fluticasone or albuterol. In addition, a combination aerosol was formed by drying agglomerates of fluticasone nanoparticles in the presence of albuterol in solution. Powders of the single d... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284008 Wed, 21 Sep 2011 04:00:00 +0100 5284008 http://www.medworm.com/index.php?rid=5284014&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21945487%26dopt%3DAbstract Authors: Karalis V, Symillides M, Macheras P Abstract Recently, the European Medicines Agency (EMA) issued a new guideline on the investigation of bioequivalence (BE). In case of highly variable drugs, this guideline proposes that the acceptance limits for C(max) can gradually be expanded as a function of within-subject variability (CV(wR)). Actually, these BE limits exhibit leveling-off properties since they are not allowed to scale continuously, but only up to CV(wR)=50%. To avoid the risk of accepting two drug products which may differ significantly, this EMA guideline also proposes the use of a secondary constraint criterion on the geometric mean ratio (GMR) of the two products under comparison. Aim of this study was to explore the leveling-off properties of the new EMA limits ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284014 Fri, 16 Sep 2011 04:00:00 +0100 5284014 http://www.medworm.com/index.php?rid=5284013&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21945488%26dopt%3DAbstract In conclusion, fluvastatin interacts with NTCP at the level of the bile acid binding pocket and is an NTCP substrate. However, under normal conditions, NTCP-mediated uptake of this drug seems not to be a significant hepatocellular uptake pathway. PMID: 21945488 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284013 Fri, 16 Sep 2011 04:00:00 +0100 5284013 http://www.medworm.com/index.php?rid=5284012&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21946258%26dopt%3DAbstract Authors: Arouri A, Mouritsen OG Abstract A novel approach to anticancer drug delivery is presented based on lipid-like liposome-forming anticancer prodrugs that are susceptible to secretory phospholipase A(2) (sPLA(2)) that is overexpressed in several cancer types. The approach provides a selective unloading of anticancer drugs at the target tissues, as well as circumvents the necessity for "conventional" drug loading. In our attempts to improve the performance of the liposomes in vivo, several PEGylated and non-PEGylated liposomal formulations composed of a retinoid prodrug premixed with the sPLA(2)-hydrolyzable DPPC (1,2-dipalmitoyl-sn-glycero-3-phosphocholine) were prepared. Besides favorably modifying the physicochemical properties of the liposomes, the incorporation of DPPC an... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284012 Fri, 16 Sep 2011 04:00:00 +0100 5284012 http://www.medworm.com/index.php?rid=5284011&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21946259%26dopt%3DAbstract Authors: Chen ML, Shah VP, Crommelin DJ, Shargel L, Bashaw D, Bhatti M, Blume H, Dressman J, Ducharme M, Fackler P, Hyslop T, Lutter L, Morais J, Ormsby E, Thomas S, Tsang YC, Velagapudi R, Yu LX Abstract Regulatory approaches for evaluating therapeutic equivalence of multisource (or generic) drug products vary among different countries and/or regions. Harmonization of these approaches may decrease the number of in vivo bioequivalence studies and avoid unnecessary drug exposure to humans. Global harmonization for regulatory requirements may be promoted by a better understanding of factors underlying product performance and expectations from different regulatory authorities. This workshop provided an opportunity for pharmaceutical scientists from academia, industry and regulatory ag... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284011 Fri, 16 Sep 2011 04:00:00 +0100 5284011 http://www.medworm.com/index.php?rid=5284006&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21946260%26dopt%3DAbstract Authors: Abashzadeh S, Dinarvand R, Sharifzadeh M, Hassanzadeh G, Amini M, Atyabi F Abstract The novel physical hydrogels composed of chitosan or its water soluble derivatives such as carboxymethyl chitosan (CMCh) and sodium carboxymethyl chitosan (NaCMCh) and opened ring polyvinyl pyrrolidone (OP-PVP) were used as a controlled delivery system for triptorelin acetate, a luteinizing-releasing hormone agonist. The in situ gel forming system designed according to physical interactions such as chains entanglements and hydrophilic attractions especially h-bonds of chitosan and/or NaCMCh and OR-PVP. In order to increase in situ gel forming rate the chitosan microspheres prepared through spray drying technique. The chitosan or NaCMCh/OR-PVP blends prepared at different ratios (0.05, 0.10,... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5284006 Fri, 16 Sep 2011 04:00:00 +0100 5284006 http://www.medworm.com/index.php?rid=5249647&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21933707%26dopt%3DAbstract Authors: Gabizon A, Shmeeda H, Grenader T Abstract We review here various pharmacological aspects of pegylated liposomal doxorubicin (PLD) which have important implications on the safety and efficacy profile of this important agent. Particularly, the formulation properties of PLD and its long circulation time and the relationship between the high microvascular permeability of tumors and the selective accumulation of PLD in tumors are addressed. Emphasis is given to the correlation of pharmacokinetic parameters with pharmacodynamic effects of PLD. The evidence for drug interference with PLD clearance and its clinical relevance are discussed. We propose a simplified plasma PLD testing protocol for monitoring PLD clearance, as a tool for the clinician to control the safety and therape... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5249647 Sat, 10 Sep 2011 04:00:00 +0100 5249647 http://www.medworm.com/index.php?rid=5249646&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21939759%26dopt%3DAbstract This study indicates that 4,5-bisaryl imidazolyl imidazole is a suitable scaffold to design COX-2 inhibitors and 4,5-bis(4-methoxyphenyl)-1H-imidazol-2-yl derivative exhibited highly COX-2 inhibitory potency and selectivity even more than celecoxib. It seems that it could induce apoptosis in Caco-2 colorectal carcinoma cell line. PMID: 21939759 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5249646 Sat, 10 Sep 2011 04:00:00 +0100 5249646 http://www.medworm.com/index.php?rid=5234885&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21925600%26dopt%3DAbstract Authors: Maru SM, de Matas M, Kelly A, Paradkar A Abstract The influence of antiretroviral drugs and plasticizers on the rheological and thermal characteristics of ethyl cellulose formulations intended for hot melt extrusion has been investigated. Antiretroviral drugs used were zidovudine and lamivudine, whilst plasticizers included triethylcitrate (TEC) and polyethylene glycol (PEG-6000). Physical mixtures containing ethyl cellulose with varying concentrations of drugs and plasticizers were characterized using differential scanning calorimetry (DSC) and parallel plate oscillatory rheometry. The viscosity of physical mixtures containing both drugs was lower than observed for pure ethyl cellulose, indicating that the drugs had a plasticizing effect. This was confirmed by lowering of... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5234885 Sat, 10 Sep 2011 04:00:00 +0100 5234885 http://www.medworm.com/index.php?rid=5234888&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21924353%26dopt%3DAbstract Authors: Rocha NF, Oliveira GV, Araújo FY, Rios ER, Carvalho AM, Soares PM, Sousa DP, Sousa FC Abstract This work examined the gastroprotection of (-)-α-bisabolol, an unsaturated optically active sesquiterpene alcohol obtained by the direct distillation essential oil from plants. (-)-α-Bisabolol has been described as a compound capable of reducing the gastric ulcer area in response to absolute ethanol. We evaluated the gastroprotection of (-)-α-bisabolol in ethanol-induced gastric lesions model through histopathological assessment, measurement of the membrane lipids peroxidation (MDA), myeloperoxidase (MPO) activity, superoxide dismutase (SOD) activity, catalase (CAT) activity and the nitrite amount. Our results showed that (-)-α-bisabolol was able to reduce injuries associate... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5234888 Thu, 08 Sep 2011 04:00:00 +0100 5234888 http://www.medworm.com/index.php?rid=5234887&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21925598%26dopt%3DAbstract Authors: Dube A, Nicolazzo JA, Larson I Abstract The green tea catechin (-)-epigallocatechin gallate (EGCG) has attracted significant research interest due to its beneficial therapeutic effects, which include anti-oxidant, neuro-protective and anti-cancer effects. However, the therapeutic potential of EGCG following oral consumption is limited by its poor absorption. To address this issue, EGCG has been encapsulated in chitosan-tripolyphosphate nanoparticles (CS NPs) and the oral absorption of EGCG evaluated in Swiss Outbred mice. Administration of the CS NPs enhanced the plasma exposure of total EGCG by a factor of 1.5 relative to an EGCG solution, with plasma AUC((0-5h)) values of 116.4±4.1 and 179.3±10.8nM.h (mean±s.d., n=3-5) for the EGCG solution and CS NPs, respectively. A... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5234887 Thu, 08 Sep 2011 04:00:00 +0100 5234887 http://www.medworm.com/index.php?rid=5234886&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21925599%26dopt%3DAbstract Authors: Varkouhi AK, Mountrichas G, Schiffelers RM, Lammers T, Storm G, Pispas S, Hennink WE Abstract Cationic polymers have been studied for nucleic acid delivery both in vitro and in vivo. However, many polymer-based formulations suffer from lack of stability in biologic fluids due to interactions with anionic biomacromolecules such as proteins and polysaccharides. Likely, the stronger the electrostatic interactions between a cationic polymer and nucleic acids, the higher the stability of the polyplexes in biologic fluids will be. To get evidence for this hypothesis, quaternized poly[3,5-bis(dimethylaminomethylene)-p-hydroxyl styrene] (QNPHOS) with two permanently charged cationic sites per monomer unit as well as its block copolymer with PEG were synthesized and compared with t... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5234886 Thu, 08 Sep 2011 04:00:00 +0100 5234886 http://www.medworm.com/index.php?rid=5234884&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21925601%26dopt%3DAbstract Authors: Jacobsen JK, Jensen B, Skonberg C, Hansen SH, Badolo L Abstract The organic cation transporter 1 (Oct1) has been shown to be one of the most abundant uptake transporters responsible for the uptake of xenobiotics from the sinusoidal blood across the basolateral membrane of hepatocytes. On the same membrane the multidrug resistance-associated protein 3 (Mrp3) mediates the efflux of xenobiotics or their metabolites from the hepatocytes to the blood allowing their systemic exposure. In the present study we investigated the expression and activity of Oct1 and Mrp3 in suspensions and in monolayer- and sandwich cultures, and activities of CYP2B1/2, 2D1, and 3A1 in monolayer- and sandwich cultures of cryopreserved rat hepatocytes. Oct1-mediated active uptake of 10μM [(3)H]-1-meth... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5234884 Thu, 08 Sep 2011 04:00:00 +0100 5234884 http://www.medworm.com/index.php?rid=5221456&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21914476%26dopt%3DAbstract CONCLUSIONS: These results suggested that resveratrol attenuates acute hypoxic injury in cardiomyocytes, and the mechanism might be associated with inhibition of iNOS-NO signaling pathway via HIF-1α. PMID: 21914476 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221456 Mon, 05 Sep 2011 04:00:00 +0100 5221456 http://www.medworm.com/index.php?rid=5221455&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21914477%26dopt%3DAbstract Authors: Zhu QC, Wang Y, Liu YP, Zhang RQ, Li X, Su WH, Long F, Luo XD, Peng T Abstract In recent years, enterovirus 71 (EV71) infections have caused an increasing epidemic in young children, accompanying with more severe nervous system disease and more deaths. Unfortunately, there is no specific medication for it so far. Here we investigated the anti-EV71 activity of chrysosplenetin and penduletin, two o-methylated flavonols isolated from the leaves of Laggera pterodonta. These two compounds were found to have strong activity in vitro against EV71 with low cytotoxicity. In the cytopathic effect (CPE) inhibition assays, both plaque reduction assay and virus yield inhibition assay, the compounds showed a similar 50% inhibitory concentration (IC(50)) value of about 0.20μM. The selec... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221455 Mon, 05 Sep 2011 04:00:00 +0100 5221455 http://www.medworm.com/index.php?rid=5221462&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21907794%26dopt%3DAbstract Authors: Sonje VM, Kumar L, Puri V, Kohli G, Kaushal AM, Bansal AK Abstract Amorphous systems have gained importance as a tool for addressing delivery challenges of poorly water soluble drugs. A careful assessment of thermodynamic and kinetic behavior of amorphous form is necessary for successful use of amorphous form in drug delivery. The present study was undertaken to evaluate effect of monovalent sodium (Na(+); ATV Na), and bivalent calcium (Ca(2+); ATV Ca) and magnesium (Mg(2+); ATV Mg) counterions on properties of amorphous salts of atorvastatin (ATV) model drug. Amorphous form was generated from crystalline salts of ATV by spray drying, and characterized for glass transition temperature (T(g)), fragility and devitrification tendency. In addition, chemical stability of the am... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221462 Thu, 01 Sep 2011 04:00:00 +0100 5221462 http://www.medworm.com/index.php?rid=5221461&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21907795%26dopt%3DAbstract The objective of this study was to investigate the effect of BA on endothelium-dependent vasorelaxation in isolated aortic rings from l-NAME-induced hypertensive rats and its underlying mechanisms. Male Sprague-Dawley rats were injected with l-NAME (15mg/kg/d, i.p.) for 4weeks to induce hypertension. After treatment with l-NAME for 2weeks, rats with mean blood pressure >120mm Hg measured by tail-cuff method were considered hypertensive and then injected with BA (0.8, 4, 20mg/kg/d, i.p.) for the last 2weeks. The effect of BA on the tension of rat thoracic aortic rings was measured in an organ bath system. The levels of nitric oxide (NO), reactive oxygen species (ROS), and the activity of superoxide dismutase (SOD) and NOS in aortas were assayed. We found that BA (0.1-100μM) evoked a con... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221461 Thu, 01 Sep 2011 04:00:00 +0100 5221461 http://www.medworm.com/index.php?rid=5221460&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21907796%26dopt%3DAbstract Authors: Kunjachan S, Blauz A, Moeckel D, Theek B, Kiessling F, Etrych T, Ulbrich K, Bloois LV, Storm G, Bartosz G, Rychlik B, Lammers T Abstract Over the past few decades, many different types of nanomedicines have been evaluated, both in vitro and in vivo. In general, nanomedicines are designed to improve the in vivo properties of low-molecular-weight (chemo-) therapeutic drugs, i.e. their biodistribution and the target site accumulation, and to thereby improve the balance between their efficacy and toxicity. A significant number of studies have also addressed the in vitro properties of nanomedicines, showing e.g. their ability to overcome cellular multidrug resistance (MDR). Particularly promising results in this regard have been reported for 'pharmacologically active' carrier m... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221460 Thu, 01 Sep 2011 04:00:00 +0100 5221460 http://www.medworm.com/index.php?rid=5221459&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21907797%26dopt%3DAbstract This study therefore demonstrates that, in contrast to colchicine, these novel PEGylated colchicine-derived prodrugs are retained within the aqueous interior after encapsulation into liposomes, and that the release of the active parent can be controlled by using different biodegradable linkers. PMID: 21907797 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221459 Thu, 01 Sep 2011 04:00:00 +0100 5221459 http://www.medworm.com/index.php?rid=5221458&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21907798%26dopt%3DAbstract In this study, polymeric dispersions composed of methylcellulose (MC) and either kappa carrageenan (KC) or iota carrageenan (IC) were proposed as a platform for transscleral delivery of macromolecules. The additive effects of the two polymers were investigated using oscillatory rheometer and FT-IR spectroscopy. Mechanical spectra demonstrated a conformation dependent association of the two polymers at 37°C in the presence of selected counter ions. The polymer association was also confirmed by the shifts in MC peaks at 1049.5, 1114 and 1132.9cm(-1) in the presence of carrageenans, which corresponds to the stretching vibrations of C-O-C bonds of the polysaccharides. The MC-IC polymeric system displayed the highest bio-adhesion, owing to the relatively high negative charge. However, the MC-I... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221458 Thu, 01 Sep 2011 04:00:00 +0100 5221458 http://www.medworm.com/index.php?rid=5221457&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21907799%26dopt%3DAbstract In this study, the distribution of endogenous zinc, the disposition after intravenous injection, and the intestinal absorption of zinc were investigated in vivo using rats from the viewpoints of pharmaceutical science and pharmacokinetics. High levels of endogenous zinc were observed in bone, testis, and liver. RT-PCR analysis on the mRNA of metallothionein in tissues clarified that it is significantly correlated with the distribution of zinc, suggesting that zinc is accumulated in tissues as a complex with MT. Following intravenous injection, uptake of zinc was high in liver, spleen, pancreas, kidney, and intestine. Fractional absorptions of zinc after oral administration to fasted rats were greater than those to fed rats, suggesting that some factors in diet inhibit the absorption of zin... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221457 Thu, 01 Sep 2011 04:00:00 +0100 5221457 http://www.medworm.com/index.php?rid=5221465&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21896328%26dopt%3DAbstract Authors: Cittadino E, Ferraretto M, Torres E, Maiocchi A, Crielaard BJ, Lammers T, Storm G, Aime S, Terreno E Abstract The design of long circulating liposomes co-loaded with the glucocorticoid prednisolone phosphate (PLP) and the amphiphilic paramagnetic contrast agent Gd-DOTAMA(C(18))(2) allowed the MRI-guided in vivo visualization of the delivery and biodistribution of PLP, as well as the monitoring of drug efficacy. The performance of this theranostic probe was investigated in a mouse model bearing a melanoma B16 syngeneic tumor. The release kinetics of the drug were evaluated in vitro where it displayed a peculiar behavior characterized by a fast process (completed in few hours) involving only a small portion (<5%) of the drug. Interestingly, the incorporation of the amphip... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221465 Sun, 28 Aug 2011 04:00:00 +0100 5221465 http://www.medworm.com/index.php?rid=5221464&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21896329%26dopt%3DAbstract Authors: Arima H, Tsutsumi T, Yoshimatsu A, Ikeda H, Motoyama K, Higashi T, Hirayama F, Uekama K Abstract In the present study, we prepared the small interfering RNA (siRNA) complexes with polyamidoamine (PAMAM) dendrimer (G3) conjugate with α-cyclodextrin (α-CDE (G3)), and examined the physicochemical properties, serum resistance, in vitro RNAi effects on endogenous gene expression, cytotoxicity, interferon response, hemolytic activity, cellular association and intracellular distribution. In addition, these results were compared to the siRNA complexes with the commercial transfection reagents such as linear polyethyleneimine (PEI), Lipofectamine™2000 (L2) and RNAiFect™ (RF). α-CDE (G3) interacted with siRNA, and suppressed siRNA degradation by serum. The siRNA complex with ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221464 Sun, 28 Aug 2011 04:00:00 +0100 5221464 http://www.medworm.com/index.php?rid=5221463&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21903163%26dopt%3DAbstract This study has investigated the utility and potential advantages of gene expression programming (GEP) - a new development in evolutionary computing for modelling data and automatically generating equations that describe the cause-and-effect relationships in a system- to four types of pharmaceutical formulation and compared the models with those generated by neural networks, a technique now widely used in the formulation development. Both methods were capable of discovering subtle and non-linear relationships within the data, with no requirement from the user to specify the functional forms that should be used. Although the neural networks rapidly developed models with higher values for the ANOVA R(2) these were black box and provided little insight into the key relationships. However, GEP,... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221463 Sun, 28 Aug 2011 04:00:00 +0100 5221463 http://www.medworm.com/index.php?rid=5221466&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21893195%26dopt%3DAbstract Authors: Weiss M, Krejcie TC, Avram MJ Abstract Although indocyanine green (ICG) has long been used for the assessment of liver function, the respective roles of sinusoidal uptake and canalicular excretion in determining hepatic ICG clearance remain unclear. Here this issue was addressed by incorporating a liver model into a minimal physiological model of ICG disposition that accounts of the early distribution phase after bolus injection. Arterial ICG concentration-time data from awake dogs under control conditions and from the same dogs while anesthetized with 3.5% isoflurane were subjected to population analysis. The results suggest that ICG elimination in dogs is uptake limited since it depends on hepatocellular uptake capacity and on biliary excretion but not on hepatic blood f... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221466 Fri, 26 Aug 2011 04:00:00 +0100 5221466 http://www.medworm.com/index.php?rid=5221475&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21884787%26dopt%3DAbstract Authors: Arnold Y, Imanidis G, Kuentz M Abstract Simple oil formulations are widely used in oral drug delivery and the fate of these systems is governed mainly by the dispersion and digestion process. The current work aimed to study concentration effects of six poorly water-soluble drugs on the in vitro lipolysis rate of medium-chain triglycerides. The results were compared with drug effects on oil viscosity and surface tension. First the different drugs were characterized by molecular modeling and their influence on physical oil properties was assessed. Herein capillary viscosimetry was employed as well as dynamic surface tensiometry. Subsequently, an apparent in vitro lipolysis rate was determined in biorelevant medium using an automated pH stat titrator linked to a thermo-contro... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221475 Thu, 25 Aug 2011 04:00:00 +0100 5221475 http://www.medworm.com/index.php?rid=5221472&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21888966%26dopt%3DAbstract CONCLUSION: In terms of the underlying diffusion coefficient, the hitherto used measures give a relatively poor degree of quantification. In contrast, the present methods may yield direct information on the effective intercellular diffusion coefficient and hence provide additional and more precise information as to the permeability modulating effect of various substances. PMID: 21888966 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221472 Thu, 25 Aug 2011 04:00:00 +0100 5221472 http://www.medworm.com/index.php?rid=5221467&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21888971%26dopt%3DAbstract Authors: Foged C, Hansen J, Agger EM Abstract Induction of CD8(+) T-cell responses is critical for the immunological control of a variety of diseases upon vaccination. Modern subunit vaccines are based on highly purified recombinant proteins. The high purity represents a major advancement in terms of vaccine safety compared to previous vaccination strategies with live attenuated or whole killed pathogens, but typically renders vaccine antigens poorly immunogenic and insufficient in mobilizing protective immunity. Adjuvants are therefore needed in vaccine formulations to enhance, direct and maintain the immune response to vaccine antigens. However, a weakness of many adjuvants is the lack of induction of CD8(+) T-cell responses against protein antigens, which are required for protec... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221467 Thu, 25 Aug 2011 04:00:00 +0100 5221467 http://www.medworm.com/index.php?rid=5221470&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21888968%26dopt%3DAbstract Authors: Aslanidi OV, Al-Owais M, Benson AP, Colman M, Garratt CJ, Gilbert SH, Greenwood J, Holden AV, Kharche S, Kinnell E, Plein S, Stott J, Zhang H Abstract Computational models of human atrial cells, tissues and atria have been developed. Cell models, for atrial wall, crista terminalis, appendage, Bachmann's bundle and pectinate myocytes are characterised by action potentials, ionic currents and action potential duration (APD) restitution. The principal effect of the ion channel remodelling of persistent atrial fibrillation (AF), and a mutation producing familial AF, was APD shortening at all rates. Electrical alternans was abolished by the modelled action of Dronedarone. AF induced gap junctional remodelling slows propagation velocity at all rates. Re-entrant spiral waves in 2... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221470 Wed, 24 Aug 2011 04:00:00 +0100 5221470 http://www.medworm.com/index.php?rid=5221469&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21888969%26dopt%3DAbstract Authors: Geenen S, du Preez FB, Reed M, Frederik Nijhout H, Gerry Kenna J, Wilson ID, Westerhoff HV, Snoep JL Abstract One of the main pathways for the detoxification of reactive metabolites in the liver involves glutathione conjugation. Metabolic profiling studies have shown paradoxical responses in glutathione-related biochemical pathways. One of these is the increase in 5-oxoproline and ophthalmic acid concentrations with increased dosage of paracetamol. Experimental studies have thus far failed to resolve these paradoxes and the robustness of how these proposed biomarkers correlate with liver glutathione levels has been questioned. To better understand how these biomarkers behave in the glutathione system a kinetic model of this pathway was made. By using metabolic control anal... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221469 Wed, 24 Aug 2011 04:00:00 +0100 5221469 http://www.medworm.com/index.php?rid=5221468&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21888970%26dopt%3DAbstract Authors: Rolsted K, Rapin N, Steffansen B Abstract Substances that compete for the same saturable intestinal transporters may when dosed together lead to altered permeability and hence influence bioavailability. The aim was to simulate kinetic parameters, i.e. K(m) and J(max), for transporter mediated E(1)S permeability across Caco-2 cells by a combined experimental modeling approach. 4 classes of transporters were suggested to be involved in the permeability of E(1)S, i.e. apical influx (T(I)) and efflux (T(III)) as well as basolateral efflux (T(II)) and influx (T(IV)). Efflux ratio of E(1)S was determined to 6.8. E(1)S is suggested to have highest affinity to T(III). T(IV) is however suggested to be rate limiting in exsorptive P(APP) due to lower J(max) of T(IV), compared to T(II... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221468 Wed, 24 Aug 2011 04:00:00 +0100 5221468 http://www.medworm.com/index.php?rid=5221474&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21884788%26dopt%3DAbstract In this study; a natural polymer (poly(3-hydroxybutyrate-co-3-hydroxyhexanoate), PHBHHX) was used as a base matrix for the production of a novel nanotherapeutic including antineoplastic agent, Etoposide and attached folic acid as a ligand on the nanoparticles. Modified solvent evaporation technique was used for the production of PHBHHX nanoparticles and the average size of the obtained PHBHHX nanoparticles were observed in the range of 180nm and 1.5μm by the change in experimental conditions (i.e., homogenization rate, surfactant concentration and polymer/solvent ratio). By the increase in homogenization rate and surfactant concentration, size of the nanoparticles was decreased, while the size was increased by the increase in polymer/solvent ratio. Drug loading ratio was also found to be ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221474 Tue, 23 Aug 2011 04:00:00 +0100 5221474 http://www.medworm.com/index.php?rid=5221473&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21884789%26dopt%3DAbstract Authors: Karmwar P, Boetker J, Graeser K, Strachan C, Rantanen J, Rades T Abstract Amorphous forms of indomethacin have previously been prepared using various preparation techniques and it could be demonstrated that the way the material was prepared influenced the physicochemical properties of the amorphous form of the drug. The aim of this study was to use one preparation technique (transformation via the melt) to prepare amorphous indomethacin and to investigate the influence of the cooling rate (as a processing parameter) on the physical stability of the resulting amorphous form. The amorphous materials obtained were analysed for their structural characteristics using Raman spectroscopy in combination with multivariate data analysis. The onset of crystallisation was determined a... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221473 Tue, 23 Aug 2011 04:00:00 +0100 5221473 http://www.medworm.com/index.php?rid=5221471&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21888967%26dopt%3DAbstract In conclusion, molecular modeling elucidates the formation of the inclusion complex, stabilized through hydrogen bonds, and the encapsulation of β-lap and β-lap:HPβ-CD into liposomes could provide an alternative means leading eventually to its use in cancer research. PMID: 21888967 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5221471 Tue, 23 Aug 2011 04:00:00 +0100 5221471 http://www.medworm.com/index.php?rid=5180256&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21878388%26dopt%3DAbstract Authors: Chansanroj K, Petrović J, Ibrić S, Betz G Abstract Artificial neural networks (ANNs) were applied for system understanding and prediction of drug release properties from direct compacted matrix tablets using sucrose esters (SEs) as matrix-forming agents for controlled release of a highly water soluble drug, metoprolol tartrate. Complexity of the system was presented through the effects of SE concentration and tablet porosity at various hydrophilic-lipophilic balance (HLB) values of SEs ranging from 0 to 16. Both effects contributed to release behaviors especially in the system containing hydrophilic SEs where swelling phenomena occurred. A self-organizing map neural network (SOM) was applied for visualizing interrelation among the variables and multilayer perceptron neur... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5180256 Mon, 22 Aug 2011 23:00:00 +0100 5180256 http://www.medworm.com/index.php?rid=5180258&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21871958%26dopt%3DAbstract Authors: Veldre K, Actiņš A, Jaunbergs J Abstract The thermodynamic stability of detomidine hydrochloride monohydrate has been evaluated on the basis of phase transition kinetics in solid state. A method free of empirical models was used for the treatment of kinetic data, and compared to several known solid state kinetic data processing methods. Phase transitions were monitored by powder X-ray diffraction (PXRD) and thermal analysis. Full PXRD profiles were used for determining the phase content instead of single reflex intensity measurements, in order to minimize the influence of particle texture. We compared the applicability of isothermal and nonisothermal methods to our investigation of detomidine hydrochlorine monohydrate dehydration. PMID: 21871958 [PubMed - as supplied... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5180258 Thu, 18 Aug 2011 23:00:00 +0100 5180258 http://www.medworm.com/index.php?rid=5180257&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21871959%26dopt%3DAbstract Authors: Yen GC, Chen YL, Sun FM, Chiang YL, Lu SH, Weng CJ Abstract Lung cancer is the major cause of tumor-related death, and approximately 70% of lung cancer patients die from metastasis. Evidence that phenolic compounds may have a potential inhibitory effect on cancer invasion and metastasis is increasingly being reported in the scientific literature. Cinnamic acid is a member of phenolics which having several isoforms in nature. The trans-cinnamic acid (t-CA) has been investigated extensively for its potential pharmacological effects whereas the study of cis-cinnamic acid (c-CA) is limited because pure c-CA was hard to obtain. We had developed a practicable method previously to transform and obtain pure c-CA, and the pure compound was used to evaluate the anti-invasive effect ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5180257 Thu, 18 Aug 2011 23:00:00 +0100 5180257 http://www.medworm.com/index.php?rid=5160296&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21864677%26dopt%3DAbstract Authors: Helbling IM, Cabrera MI, Luna JA Abstract A mathematical modeling of controlled release of drug from one-layer and two-layer torus-shaped devices with external mass transfer resistance is presented. Analytical solutions based on the pseudo-steady state approximation are derived. The validity of the equations is established in two stages. In the first stage, the validity of the models derived for more complex systems is determined by comparison with profiles predicted by the simplest model, in asymptotic cases. In the second stage, the reliability and usefulness of the models are ascertained by comparison of the simulation results with vaginal rings experimental release data reported in the literature. In order to measures quantitatively the fit of the theoretical models to... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5160296 Mon, 15 Aug 2011 23:00:00 +0100 5160296 http://www.medworm.com/index.php?rid=5160295&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21864678%26dopt%3DAbstract Authors: Anwar M, Warsi MH, Mallick N, Akhter S, Gahoi S, Jain GK, Talegaonkar S, Ahmad FJ, Khar RK Abstract A novel approach to improve the bioavailability and stability of atorvastatin (AT) was developed by constructing a nano-sized polymer-atorvastatin conjugate. Firstly, a novel chitosan-atorvastatin (CH-AT) conjugate was efficiently synthesized through amide coupling reaction. The formation of conjugate was confirmed by (1)H NMR and FT-IR spectrometry. Nano-sized conjugate with a mean size of 215.3±14.2nm was prepared by the process of high pressure homogenization (HPH). Scanning electron microscopy (SEM) revealed that CH-AT nano-conjugate possess smooth surface whereas X-ray diffraction (XRD) spectra demonstrated amorphous nature of nano-conjugate. Further, CH-AT nano-conjug... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5160295 Mon, 15 Aug 2011 23:00:00 +0100 5160295 http://www.medworm.com/index.php?rid=5160294&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21864679%26dopt%3DAbstract Authors: Velický M, Tam KY, Dryfe RA Abstract The purpose of this study was to develop an in vitro permeation model that will predict the fraction of drugs absorbed in humans. A rotating-diffusion cell with two aqueous compartments, separated by a lipid-impregnated artificial membrane, was used to determine the permeability of drugs under conditions of controlled hydrodynamics. The measured effective permeability coefficient was modified to include the paracellular transport derived from a previously reported colorectal adenocarcinoma epithelial cell line (Caco-2) permeability study and the effects of unstirred water layer anticipated in vivo. Permeability data were collected for 31 different marketed drugs with known absolute oral bioavailability and human hepatic clearance data.... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5160294 Mon, 15 Aug 2011 23:00:00 +0100 5160294 http://www.medworm.com/index.php?rid=5160299&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21854846%26dopt%3DAbstract The objective was to estimate how important CYP2C19 and CYP2D6 phenotype status, hepatic activity of CYP3A4, body weight, CYP2D6 phenotype dose adjustment, and drug-drug interactions are with regard to accidental poisoning in a virtual population receiving a daily dose of 100mg nortriptyline. Accidental poisoning is here defined as intake of a normal dose which because of slow metabolism may lead to potentially toxic concentrations. The input parameters values for Simcyp were based on average literature in vitro and in vivo data. The Simcyp simulations of nortriptyline pharmacokinetics reflected reported clinical concentration-time profiles, therapeutic drug monitoring data, and the consequence of CYP2D6 poor metaboliser (PM) and ultrarapid metaboliser status. Of the investigated factors, ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5160299 Wed, 10 Aug 2011 23:00:00 +0100 5160299 http://www.medworm.com/index.php?rid=5160297&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21856416%26dopt%3DAbstract The objectives of this paper were to analyze these systems from a mathematical/analytical and quantitative point of view and to present simulations with different parameter settings and dosing regimens in order to highlight the intrinsic behaviour of these systems and to present expressions and graphs that are applicable for quantification of rate and extent of tolerance and rebound. The dynamics of the moderators (k(tol)) compared to the dynamics of the response (k(out)), was shown to be important for the behaviour of both systems. For instance, slow dynamics of the moderator compared to the response (k(tol)<<k(out)), resulted in overshoot and pronounced rebound. The extent of tolerance was studied over time at a single constant drug concentration and at steady state for different d... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5160297 Wed, 10 Aug 2011 23:00:00 +0100 5160297 http://www.medworm.com/index.php?rid=5160298&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21855632%26dopt%3DAbstract Authors: Lv P, Fang W, Geng X, Yang Q, Li Y, Sha L Abstract Cerebral ischemia and reperfusion is one of the leading causes for death and severe disabilities in the world and often lead to irreversible brain damage over later lifespan. The aim of this study was to investigate the evolution of pathological damage in cerebral cortex and basal ganglia following ischemia and to evaluate the therapeutic neuroprotective effect of ginkgolide B in a rat model of stroke induced by middle cerebral artery occlusion (MCAO). TTC stain, brain water content and Evans-Blue extravagation were used to quantify brain damage. Our results demonstrated that basal ganglia undergo progressive pathological damage earlier following MCAO, and injury was stable and irreversible after 5h following ischemia. How... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5160298 Tue, 09 Aug 2011 23:00:00 +0100 5160298 http://www.medworm.com/index.php?rid=5142672&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21839830%26dopt%3DAbstract Authors: Petrović J, Chansanroj K, Meier B, Ibrić S, Betz G Abstract Various modeling techniques have been applied to analyze fluidized-bed granulation process. Influence of various input parameters (product, inlet and outlet air temperature, consumption of liquid-binder, granulation liquid-binder spray rate, spray pressure, drying time) on granulation output properties (granule flow rate, granule size determined using light scattering method and sieve analysis, granules Hausner ratio, porosity and residual moisture) has been assessed. Both conventional and novel modeling techniques were used, such as screening test, multiple regression analysis, self-organizing maps, artificial neural networks, decision trees and rule induction. Diverse testing of developed models (internal and ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5142672 Wed, 03 Aug 2011 23:00:00 +0100 5142672 http://www.medworm.com/index.php?rid=5142671&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21839831%26dopt%3DAbstract Authors: Samadder A, Chakraborty D, De A, Bhattacharyya SS, Bhadra K, Khuda-Bukhsh AR Abstract We injected alloxan (100mg/perkgb.w.) in mice (Mus musculus) intra-peritoneally to induce hyperglycemia and divided the hyperglycemic mice into two sub-groups: one was fed ethanolic extract of Syzygium jambolanum (EESJ) (20mg/kgb.w. for 8weeks) and the other 85% ethyl alcohol ("vehicle"-control). Chromatographic and mass spectroscopic studies of EESJ revealed two principal components, one corresponding to an iridoid glycoside. We estimated blood glucose, glycosylated hemoglobin, glucokinase, and fructosamine and analyzed the expression of marker proteins like insulin, GLUT2, and GLUT4. We also studied anti-oxidant biomarkers like lipid peroxidase, superoxide dismutase, total thiole and ca... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5142671 Wed, 03 Aug 2011 23:00:00 +0100 5142671 http://www.medworm.com/index.php?rid=5142670&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21839832%26dopt%3DAbstract Authors: Lukáč M, Prokipčák I, Lacko I, Devínsky F Abstract The solubilisation of three natural compounds, griseofulvin and rutin, in micellar solutions of mixtures of gemini (N,N'-didecyl-N,N,N',N'-tetramethylethane-1,2-diyldiammonium dibromide) and heterogemini (decyl 2-[decyl(dimethyl)ammonio]ethylphosphate) surfactants has been studied. The highest solubilisation capacities were found for mixtures with a molar fraction of heterogemini surfactant equal or greater than the molar fraction of gemini surfactant. The relationship between synergism in surface properties of mixtures of surfactants and their solubilisation properties was also investigated. PMID: 21839832 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5142670 Wed, 03 Aug 2011 23:00:00 +0100 5142670 http://www.medworm.com/index.php?rid=5110851&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21820509%26dopt%3DAbstract Authors: Puras G, Salvador A, Igartua M, Hernández RM, Pedraz JL The aim of the present work was to develop an easy, safe and effective vaccine in Balb/c mice using the Aβ(1-15) peptide as immunogen entrapped in PLGA microparticles to reduce the risk of an adverse T cell-mediated response. Aβ(1-15,) which contains the N-terminal antibody epitope of the full Aβ(1-42) peptide was encapsulated in PLGA by a modified solvent evaporation/extraction technique using a double emulsion system. Microparticles were characterized in terms of size distribution (1.22±0.28μm), encapsulation efficiency (75.05±4.17%), surface associated peptide (59.81±0.96%) and "in vitro" release profile. Balb/c mice were immunized by subcutaneous and intranasal routes with three 30μg doses of the peptide micr... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110851 Tue, 26 Jul 2011 23:00:00 +0100 5110851 http://www.medworm.com/index.php?rid=5110852&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21803154%26dopt%3DAbstract Authors: Gonzalez-Gonzalez M, Jara-Acevedo R, Matarraz S, Jara-Acevedo M, Paradinas S, Sayagües JM, Orfao A, Fuentes M The field of proteomics has undergone rapid advancements over the last decade and protein microarrays have emerged as a promising technological platform for the challenging tasks of studying complex proteomes. Researchers have gone beyond traditional techniques and approached promising disciplines like nanotechnology to satisfy the growing demands of studying proteins in high-throughput format. Applications of nanotechnology in proteomics came from the need to detect low-abundant proteins in complex mixtures for sensitive, real-time and multiplexed detection platform. The scope of this article is to outline the current status and key technological advances of nanotech... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110852 Thu, 21 Jul 2011 23:00:00 +0100 5110852 http://www.medworm.com/index.php?rid=5110853&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21787865%26dopt%3DAbstract Authors: Koller DM, Hannesschläger G, Leitner M, Khinast JG Optical coherence tomography (OCT) is a non-invasive analysis technique allowing fast and high-quality cross-sectional imaging of scattering media. OCT is based on the physical phenomenon of low coherence interferometry and is thus well suited to image layered structures. In this paper, high-speed spectral domain OCT was used for the characterization of pharmaceutical tablet coatings, sampled at different stages of an industrial drum spray coating process, comprising tablets with a coating thickness ranging from uncoated to a target coating thickness of about 70μm. In addition to the OCT investigation of layer thickness and homogeneity, tablet weight gain and tablet diameters were determined on a single-tablet level. Scannin... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110853 Tue, 19 Jul 2011 23:00:00 +0100 5110853 http://www.medworm.com/index.php?rid=5110858&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21782938%26dopt%3DAbstract Authors: Bjerrum OJ This commentatory should be read in connection with the subsequent article about current trends in the evolvement of the pharmaceutical industries. It points to importance for the industries to have access to pharmaceutical sciences researchers educated and trained at the highest level through the newly established public-private system of courses in Europe supported by EU. PMID: 21782938 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110858 Sun, 17 Jul 2011 23:00:00 +0100 5110858 http://www.medworm.com/index.php?rid=5110857&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21782939%26dopt%3DAbstract This study showed that the therapy with DOX-Lf-PCLs offers an effective therapeutic potential for gliomas. PMID: 21782939 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110857 Sun, 17 Jul 2011 23:00:00 +0100 5110857 http://www.medworm.com/index.php?rid=5110855&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21782941%26dopt%3DAbstract Authors: Rusu A, Kuokkanen K, Heier A This commentary offers an overview of some current trends of the pharmaceutical industry drawing on examples taken from the analysis of four companies (Pfizer, Merck, Novo Nordisk, Crucell). The very brief analysis looks at diversification paths, pipeline management strategies, generic competition as well as corporate social responsibility policies. PMID: 21782941 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110855 Sun, 17 Jul 2011 23:00:00 +0100 5110855 http://www.medworm.com/index.php?rid=5110856&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21782940%26dopt%3DAbstract This article has been withdrawn at the request of the author(s) and/or editor. The Publisher apologizes for any inconvenience this may cause. The full Elsevier Policy on Article Withdrawal can be found at http://www.elsevier.com/locate/withdrawalpolicy. PMID: 21782940 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110856 Wed, 13 Jul 2011 23:00:00 +0100 5110856 http://www.medworm.com/index.php?rid=5110863&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21767640%26dopt%3DAbstract Authors: Kumar L, Baheti A, Mokashi A, Bansal AK This manuscript studies the effect of counterion on the phase behaviour during lyophilization of indomethacin salts. Salt forms of indomethacin namely, sodium, potassium, rubidium and cesium were prepared in situ and analyzed by modulated differential scanning calorimetry (MDSC) for determination of the critical process parameter for lyophilization. At a cooling rate of 17°C/min, indomethacin salts separated as amorphous form on freeze concentration. Tg' of indomethacin salts followed the order: sodium (-35.36°C)>potassium (-38.90°C)>rubidium (-43.70°C)>cesium (-47.84°C) salt. Tg' was followed by crystallization exotherm during the heating run for all salts, except indomethacin cesium. At slower cooling rates (0.5 and 1°C/... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110863 Tue, 12 Jul 2011 23:00:00 +0100 5110863 http://www.medworm.com/index.php?rid=5110862&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21777676%26dopt%3DAbstract Authors: Granath B, Holgersson J, Brenden N Immunogenicity is a continuous efficacy and safety issue of biopharmaceuticals. Pre-clinical models for prediction of immunogenicity itself as well as biomarkers to reveal potential mechanisms behind an already existing antibody response are still needed. A sensitive, robust and specific immunogenicity assay has therefore been developed that can detect and measure antibodies of five classes against an administered recombinant human protein drug. Additionally, a validation was performed to evaluate the reproducibility and specificity of this newly developed assay. The production of drug-induced antibodies in mice injected with a recombinant human protein drug has been measured by using a modified version of a multi-parametric bead analysis tec... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110862 Mon, 11 Jul 2011 23:00:00 +0100 5110862 http://www.medworm.com/index.php?rid=5110861&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21782017%26dopt%3DAbstract CONCLUSIONS: The placental transfer of repaglinide from mother to fetus was low. Since a higher transfer rate of repaglinide was observed in fetal-to-maternal than maternal-to-fetal direction, active transport by OATP-transporters may be an important factor in fetal exposure to repaglinide. PMID: 21782017 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110861 Mon, 11 Jul 2011 23:00:00 +0100 5110861 http://www.medworm.com/index.php?rid=5110860&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21782018%26dopt%3DAbstract Authors: Vo TS, Ngo DH, Ta QV, Kim SK Herpes simplex virus (HSV) is a member of the Herpesviridae family that causes general communicable infections in human populations throughout the world, the most common being genital and orolabial disease. The current treatments for HSV infections are nucleoside analogs such as acyclovir, valacyclovir and famciclovir. Despite the safety and efficacy, extensive clinical use of these drugs has led to the emergence of resistant viral strains, mainly in immunocompromised patients. To counteract these problems, alternative anti-HSV agents from natural products have been reported. Recently, a great deal of interest has been expressed regarding marine organisms such as algae, sponges, tunicates, echinoderms, mollusks, shrimp, bacteria, and fungus as prom... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110860 Mon, 11 Jul 2011 23:00:00 +0100 5110860 http://www.medworm.com/index.php?rid=5110859&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21782019%26dopt%3DAbstract Authors: Li YF, Liu ZQ The antioxidant capacities of ferrocenyl Schiff bases including o-(1-ferrocenylethylideneamino)phenol (OFP), m-(1-ferrocenylethylideneamino)phenol (MFP), and p-(1-ferrocenylethylideneamino)phenol (PFP) were evaluated in 2,2'-azobis(2-amidinopropane hydrochloride) (AAPH), Cu(2+)/glutathione (GSH), and hydroxyl radical (()OH)-induced oxidation of DNA, and in trapping 2,2'-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonate) cationic radical (ABTS(+)()), respectively. OFP, MFP and PFP possessed similar activities to trap DPPH and ABTS(+)(). All the ferrocenyl Schiff bases employed herein behaved as prooxidants in Cu(2+)/GSH- and ()OH-induced oxidation of DNA except that OFP exhibited weak antioxidant activity in ()OH-induced oxidati... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110859 Mon, 11 Jul 2011 23:00:00 +0100 5110859 http://www.medworm.com/index.php?rid=5110854&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21782942%26dopt%3DAbstract Authors: Oh EK, Jin SE, Kim JK, Park JS, Park Y, Kim CK 5-Aminolevulinic acid (5-ALA), inducing photodynamic protoporphyrin (PpIX), is a hydrophilic molecule, resulting in leashing the capacity to cross tissue barriers like stratum corneum (SC) of skin. Here, we aimed to develop 5-ALA loaded ultradeformable liposomes (UDL) with different surface charges, and to investigate their physicochemical characteristics and capability for the skin penetration and retention of 5-ALA for topical photodynamic therapy (PDT). The effects of surface charges of UDL on in vitro permeation of 5-ALA and in vivo accumulation of 5-ALA-induced PpIX in viable skin were determined and then compared with conventional neutral liposomes (nLiposome). All UDL showed smaller particle size and better deformability th... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5110854 Mon, 11 Jul 2011 23:00:00 +0100 5110854 http://www.medworm.com/index.php?rid=5018106&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21742030%26dopt%3DAbstract Authors: Wang T, Wang N, Song H, Xi X, Wang J, Hao A, Li T To enhance oral bioavailability and anti-diabetic efficacy of berberin (BER), an anhydrous reverse micelle (ARM) delivery system was prepared through lyophilization of water-in-oil (W/O) emulsions. Using soy phosphatidylcholine as emulsifiers, BER-containing W/O emulsions were prepared and then lyophilized to form dry products which, upon addition of oil, formed clear ARMs containing amorphous BER nanoparticles. BER-loaded ARMs or free BER solutions were administered to STZ-induced diabetic mice. In vivo measurements demonstrated that the blood glucose levels (BGLs) of diabetic mice reduced on average to 22% of the initial values 4h after intravenous injection of BER solution at the dose of 2.5mg/kg body weight, while the avera... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5018106 Thu, 30 Jun 2011 23:00:00 +0100 5018106 http://www.medworm.com/index.php?rid=5018107&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21740969%26dopt%3DAbstract Authors: Hao K, Gong P, Sun SQ, Hao HP, Wang GJ, Dai Y, Chen YC, Liang Y, Xie L, Li FY, Li HY We sought to develop a mechanism-based pharmacokinetic-pharmacodynamic (PK-PD) model to characterize the effects of ginsenoside Rb1 (Rb1) and estradiol (E(2)) on neural 5-hydroxytryptamine (5-HT) concentration in ovariectomized mice. PK data of Rb1 and E(2) were obtained in plasma and brain. Brain levels of 5-HT, tryptophan (TRP), 5-hydroxytryptophan (5-HTP), and 5-hydroxyindoleacetic acid (5-HIAA) were determined after a single intravenous injection of Rb1 (20mg/kg) and E(2) (0.2mg/kg) in ovariectomized mice. The activities of tryptophan hydroxylase (TPH), aromatic amino acid decarboxylase (AAAD), and monoamine oxidase (MAO) were also evaluated. Rb1 and E(2) elevated neural 5-HT levels via TP... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5018107 Tue, 28 Jun 2011 23:00:00 +0100 5018107 http://www.medworm.com/index.php?rid=5018113&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21726635%26dopt%3DAbstract Authors: Mazák K, Kökösi J, Noszál B The experimental determination of microscopic partition coefficients for protonation isomers is elaborated for the first time, and applied for niflumic acid, an ampholytic, mainly zwitterionic drug for pains in joints and muscles. The acid-base microequilibria of niflumic acid are also characterized by NMR-pH and deductive methods using auxiliary compounds of reduced complexity. The results show that 16 times as many zwitterionic than non-charged microspecies exist in aqueous solution. Partition of the individual microspecies was mimicked by model compounds of the closest possible similarity, then correction factors were also determined and introduced. Thus the long-awaited intrinsic partition coefficients of the non-charged vs. zwitterionic spe... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5018113 Fri, 24 Jun 2011 23:00:00 +0100 5018113 http://www.medworm.com/index.php?rid=5018112&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21726636%26dopt%3DAbstract Authors: Tam KY, Leung KC, Wang YX Chemoembolization has been used in the field of interventional oncology. Although practiced widely, it has only recently been demonstrated that the use of transarterial chemoembolization (TACE) provides a survival benefit based on randomized controlled trials. TACE combines the effect of targeted chemotherapy with the effect of ischemic necrosis induced by arterial embolization. Most of the TACE procedures have been based on iodized oil utilizing its microembolic and drug-carrying characteristics. Recently, there have been efforts to improve the delivery of chemotherapeutic agents to a tumor, which leads to the development of drug-eluting particles. In this review, we will describe the properties and efficacy of some chemoembolization agents which are... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5018112 Fri, 24 Jun 2011 23:00:00 +0100 5018112 http://www.medworm.com/index.php?rid=5018111&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21726637%26dopt%3DAbstract In this study, the potential of perfusion calorimetry in the characterization of solvates forming isomorphic desolvates was investigated. Perfusion calorimetry was used to expose different hydrates forming isomorphic desolvates (emodepside hydrates II-IV, erythromycin A dihydrate and spirapril hydrochloride monohydrate) to stepwise increasing relative vapour pressures (RVP) of water and methanol, respectively, while measuring thermal activity. Furthermore, the suitability of perfusion calorimetry to distinguish the transformation of a desolvate into an isomorphic solvate from the adsorption of solvent molecules to crystal surfaces as well as from solvate formation that is accompanied by structural rearrangement was investigated. Changes in the samples were confirmed using FT-Raman and FT-I... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5018111 Fri, 24 Jun 2011 23:00:00 +0100 5018111 http://www.medworm.com/index.php?rid=5018110&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21726638%26dopt%3DAbstract Authors: Pliszczak D, Bourgeois S, Bordes C, Valour JP, Mazoyer MA, Orecchioni AM, Nakache E, Lantéri P The purpose of this study was to design a new vaginal bioadhesive delivery system based on pectinate-hyaluronic acid microparticles for probiotics and prebiotics encapsulation. Probiotic strains and prebiotic were selected for their abilities to restore vaginal ecosystem. Microparticles were produced by emulsification/gelation method using calcium as cross-linking agent. In the first step, preliminary experiments were conducted to study the influence of the main formulation and process parameters on the size distribution of unloaded microparticles. Rheological measurements were also performed to investigate the bioadhesive properties of the gels used to obtain the final microparticl... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5018110 Fri, 24 Jun 2011 23:00:00 +0100 5018110 http://www.medworm.com/index.php?rid=5018109&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21726639%26dopt%3DAbstract Authors: Hüsch J, Dutagaci B, Glaubitz C, Geppert T, Schneider G, Harms M, Müller-Goymann CC, Fink L, Schmidt MU, Setzer C, Zirkel J, Rebmann H, Schubert-Zsilavecz M, Abdel-Tawab M So-called NSAID-phospholipid-complexes have been recently reported in literature to reduce local gastrointestinal toxicity. The present work was dedicated to the structural characterization of the so-called drug-phospholipid-complexes on the example of diclofenac sodium, ibuprofen and piroxicam complexes with dipalmitoylphosphatidylcholine (DPPC) at different stages of preparation. The applied techniques include (1)H/2D ROESY NMR for the structural characterization in organic solvents, FT-IR and X-ray diffraction for the structural characterization in the solid state and PCS, (31)P NMR, as well as MAS (1)H... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5018109 Fri, 24 Jun 2011 23:00:00 +0100 5018109 http://www.medworm.com/index.php?rid=5018108&cid=s_35549_13_f&fid=35549&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21726640%26dopt%3DAbstract Authors: Zidan AS, Rahman Z, Khan MA A variety of factors were systemically evaluated in order to establish the characteristics of the niosomes obtained with a high-pressure homogenizer. The vesicular sizing parameters, electrical properties, drug entrapment data and drug release characteristics were investigated using two groups of factors. The first group presented the physical process variables such as pressure of the homogenizer and the times that the samples were processed (cycles). The second group encompassed the compositional variables such as the drug loading, surfactant chain length, cholesterol level and the level of the charge imparting agent. The obtained data showed that the drug distributed within both the aqueous and lipid phases of the formed niosomes. Saturation-like ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=5018108 Fri, 24 Jun 2011 23:00:00 +0100 5018108