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. Sat, 20 Mar 2010 14:09:36 +0100 http://www.medworm.com/index.php?rid=3374920&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%3D20230893%26dopt%3DAbstract In conclusion, the crystalline and amorphous forms of CLB exhibited disparate surface milieu, which in turn can have implications on the surface mediated events. PMID: 20230893 [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=3374920 Fri, 12 Mar 2010 00:00:00 +0100 3374920 http://www.medworm.com/index.php?rid=3374919&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%3D20230894%26dopt%3DAbstract Authors: Dinunzio JC, Brough C, Miller DA, Williams RO, McGinity JW Thermal manufacturing methods for the production of solid dispersions frequently require the addition of a plasticizer in order to achieve requisite molten material flow properties when processed by unit operations such as hot melt extrusion. KinetiSol((R)) Dispersing, a rapid high energy thermal manufacturing process, was investigated for the ability to produce amorphous solid dispersions without the aid of a plasticizer. For this study itraconazole was used as a model active ingredient, while Eudragit((R)) L100-55 and Carbomer 974P were used as model solid dispersion carriers. Triethyl citrate (TEC) was used as necessary as a model plasticizer. Compositions prepared by KinetiSol((R)) Dispersing and hot melt extrusion... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3374919 Fri, 12 Mar 2010 00:00:00 +0100 3374919 http://www.medworm.com/index.php?rid=3350119&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%3D20211252%26dopt%3DAbstract Authors: Rispens T, Himly M, Heer PO, Bleker TH, Aalberse RC To prevent multimer formation, intravenous immunoglobulin (IVIG) is often treated with traces of pepsin. So far, the mechanism behind this treatment has been unclear. Recently, we reported that human IgG4 binds other IgG molecules via Fc-Fc interactions. Here we show that IVIG treated with traces of pepsin (Nanogam) inhibits these interactions. We found that-besides IgG4-peptides corresponding to IgG1 and IgG2 pFc' (products of limited pepsin digestion) are responsible for the inhibitory action. Using radiolabeled pFc', it was found that pFc' binds directly to IgG1. Furthermore, recombinant CH3 fragments were found to also possess binding activity, and potencies of inhibition varied over 3 orders of magnitude amongst the subc... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3350119 Fri, 05 Mar 2010 00:00:00 +0100 3350119 http://www.medworm.com/index.php?rid=3332011&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%3D20188824%26dopt%3DAbstract Authors: Li HY, Song X, Seville PC The use of sodium carboxymethylcellulose (NaCMC) as a spray-drying excipient in the preparation of inhalable formulations of proteins was investigated, using alkaline phosphatase as a model functional protein. Two spray-dried powders were investigated: a control powder comprising 100% w/w alkaline phosphatase and a test powder comprising 67% w/w NaCMC and 33% w/w alkaline phosphatase. Following physicochemical characterisation, the powders were prepared as both dry powder inhaler (DPI) and pressurised metered dose inhaler (pMDI) formulations. The aerosolisation performance of the formulations was assessed using a Multi-Stage Liquid Impinger, both immediately after preparation and over a 16-week storage period. Formulating the control powder as a DPI r... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3332011 Wed, 24 Feb 2010 00:00:00 +0100 3332011 http://www.medworm.com/index.php?rid=3332008&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%3D20188825%26dopt%3DAbstract Authors: Richter A, Wiedekind A, Krause M, Kissel T, Haag R, Olbrich C The purpose of this study was to investigate dendritic glycerol-based amphiphiles as novel solubilizers using poorly water-soluble anticancer drug Sagopilone. The effect of different core structures on the solubilization, formulation stability, and cytotoxicity using human umbilical vein endothelial cells (HUVEC) were investigated and compared to standard excipients. Structurally, all amphiphiles were composed of 2(nd) generation polyglycerol (PG[G2]) as the hydrophilic part and a single C(18)-chain (PG[G2]-C(18)), a C(18)-chain coupled by a diaromatic spacer (PG[G2]-DiAr-C(18)), a C(18)-chain with a naphthyl or bisphenyl end group (PG[G2]-C(18)-Naph/-BiP), or two C(18)-chains (PG[G2]-(C(18))(2)) as the hydrophobic ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3332008 Wed, 24 Feb 2010 00:00:00 +0100 3332008 http://www.medworm.com/index.php?rid=3332012&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%3D20188168%26dopt%3DAbstract In conclusion, our analysis suggested the presence of a MW cutoff for anions in dogs, which may be related with the molecular size of a compound. This represents the first report of the influence of MW or molecular volume as a determinant of biliary excretion for a structurally diverse set of compounds in dogs. PMID: 20188168 [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=3332012 Tue, 23 Feb 2010 00:00:00 +0100 3332012 http://www.medworm.com/index.php?rid=3312497&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%3D20184955%26dopt%3DAbstract This study showed that the MPEG-hexPLA micelles can be efficiently lyophilised and this process can be usefully applied to increase the pharmaceutical stability of these pharmaceutical micelle formulations. PMID: 20184955 [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=3312497 Mon, 22 Feb 2010 00:00:00 +0100 3312497 http://www.medworm.com/index.php?rid=3298739&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%3D20172026%26dopt%3DAbstract In conclusion, co-spray dried particles of ICS/LABA/M-SD were largely crystalline, stable and showed excellent aerosol performance. They may provide an attractive alternative strategy to develop combination products without lactose blends. PMID: 20172026 [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=3298739 Thu, 18 Feb 2010 00:00:00 +0100 3298739 http://www.medworm.com/index.php?rid=3298738&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%3D20172027%26dopt%3DAbstract The objective of the study was to characterise the aqueous dispersions of ritonavir melt extrudates. More specifically to look into the particular system formed when melt extrudate of a poorly soluble drug dissolved in a hydrophilic polymer matrix containing a surfactant is dispersed in an aqueous medium. Melt extrudates with and without ritonavir were studied. The drug containing extrudate was confirmed to be molecular dispersions of drug in a polymer/surfactant matrix. Particulate dispersions were formed in water from both drug and placebo extrudates. The dispersions were investigated with respect to mean particle size and particle size distribution (photon correlation spectroscopy and optical particle counting), surface charge (zeta potential), particle composition (ultracentrifugation)... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3298738 Thu, 18 Feb 2010 00:00:00 +0100 3298738 http://www.medworm.com/index.php?rid=3270291&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%3D20149867%26dopt%3DAbstract This study aimed to determine whether berberine could alleviate pro-inflammatory cytokine induced intestinal epithelial tight junction damage. Caco-2 monolayers were treated with tumor necrosis factor-alpha and interferon-gamma to induce barrier dysfunction. The protective effect of berberine on tight junctions was analyzed by measuring the transepithelial electrical resistance (TEER). Transmission electron microscopy was used to observe the morphology of tight junction, and subcellular localization of tight junction proteins was investigated by immunofluorescence microscopy and Western blot. Berberine significantly prevented pro-inflammatory cytokines induced decrease in TEER. The distortion of tight junction morphology and redistribution of tight junction protein occludin was also preven... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3270291 Mon, 08 Feb 2010 00:00:00 +0100 3270291 http://www.medworm.com/index.php?rid=3270290&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%3D20149868%26dopt%3DAbstract Authors: Huh Y, Cho HJ, Yoon IS, Choi MK, Kim JS, Oh E, Chung SJ, Shim CK, Kim DD Hyaluronic acid (HA)-based microspheres containing PEG 6000 and/or sodium taurocholate (NaTC) were prepared by the spray-drying method for nasal delivery of fexofenadine hydrochloride (HCl). Their physicochemical properties including particle size and drug contents were determined, while their morphology examined by a scanning electron microscope (SEM). The effects of the solubilizer (PEG 6000) and the permeation enhancer (NaTC) on the in vitro release characteristics of fexofenadine.HCl were observed. Moreover, the in vitro permeation of fexofenadine.HCl was determined using the human nasal cell (HNE) monolayers cultured on Transwell((R)) inserts. After nasal administration, fexofenadine.HCl in rabbit pl... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3270290 Mon, 08 Feb 2010 00:00:00 +0100 3270290 http://www.medworm.com/index.php?rid=3270292&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%3D20138213%26dopt%3DAbstract Authors: Serpe L, Canaparo R, Daperno M, Sostegni R, Martinasso G, Muntoni E, Ippolito L, Vivenza N, Pera A, Eandi M, Gasco MR, Zara GP Standard treatment for inflammatory bowel diseases (IBD) necessitates frequent intake of anti-inflammatory and/or immunosuppressive drugs, leading to significant adverse events. To evaluate the role solid lipid nanoparticles (SLN) play as drug delivery system in enhancing anti-inflammatory activity for drugs such as dexamethasone and butyrate in a human inflammatory bowel diseases whole blood model. ELISA assay and the peripheral blood mononuclear cell (PBMC) cytokine mRNA expression levels were evaluated by quantitative SYBR Green real-time RT-PCR to determine the IL-1beta, TNF-alpha, IFN-gamma and IL-10 secretion in inflammatory bowel diseases patien... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3270292 Wed, 03 Feb 2010 00:00:00 +0100 3270292 http://www.medworm.com/index.php?rid=3247305&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%3D20132884%26dopt%3DAbstract In conclusion, subcutaneous implantation of mifepristone-loaded PCL/Pluronic F68 capsules was proven an effective means for long-term treatment of chronic endometriosis. PMID: 20132884 [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=3247305 Mon, 01 Feb 2010 00:00:00 +0100 3247305 http://www.medworm.com/index.php?rid=3240206&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%3D20122569%26dopt%3DAbstract Authors: The Turkish Pharmaceutical Technology Scientists' Association Tüftad PMID: 20122569 [PubMed - in process] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3240206 Sun, 31 Jan 2010 00:00:00 +0100 3240206 http://www.medworm.com/index.php?rid=3240205&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%3D20122570%26dopt%3DAbstract Authors: Bortolotti F, Balducci AG, Sonvico F, Russo P, Colombo G PMID: 20122570 [PubMed - in process] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3240205 Sun, 31 Jan 2010 00:00:00 +0100 3240205 http://www.medworm.com/index.php?rid=3232243&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%3D20117207%26dopt%3DAbstract Authors: Ho J, Huang Y, Danquah MK, Wang H, Forde GM DNA vaccines or proteins are capable of inducing specific immunity; however, the translation to the clinic has generally been problematic, primarily due to the reduced magnitude of immune response and poor pharmacokinetics. Herein we demonstrate a composite microsphere formulation, composed of mesoporous silica spheres (MPS) and PLGA, enables the controlled delivery of a prime-boost vaccine via the encapsulation of plasmid DNA (pDNA) and protein in different compartments. Method with modified dual-concentric-feeding needles attached to a 40kHz ultrasonic atomizer was studied. These needles focus the flow of two different solutions, which passed through the ultrasonic atomizer. The process synthesis parameters, which are important to ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3232243 Thu, 28 Jan 2010 00:00:00 +0100 3232243 http://www.medworm.com/index.php?rid=3232242&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%3D20117208%26dopt%3DAbstract Authors: Jarukamjorn K, Kondo S, Chatuphonprasert W, Sakuma T, Kawasaki Y, Nemoto N We previously observed a strong synergistic effect on polycyclic aromatic hydrocarbon (PAH)-induced CYP1A1 expression by andrographolide, a major constituent of an herbal medicine derived from the plant Andrographis paniculata, in mouse hepatocytes in primary culture. The present paper describes confirmation of an enhancing effect of andrographolide on the CYP1 family in vivo in the PAH-responsive C57BL/6 mouse. Andrographolide did not alter CYP1 expression in the PAH-nonresponsive DBA/2 mouse. The enhanced expression induced by andrographolide was observed in male C57BL/6 mice, but not in intact or ovariectomized females, or in orchiectomized male mice. However, treatment with testosterone restored the... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3232242 Thu, 28 Jan 2010 00:00:00 +0100 3232242 http://www.medworm.com/index.php?rid=3221375&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%3D20109545%26dopt%3DAbstract Authors: Wauthoz N, Deleuze P, Hecq J, Roland I, Saussez S, Adanja I, Debeir O, Decaestecker C, Mathieu V, Kiss R, Amighi K The aim of this study was to compare the efficacy of local drug delivery by inhalation to intravenous delivery in a B16F10 melanoma metastatic lung model. Temozolomide was formulated as a suspension, which was elaborated and evaluated in terms of particle size, shape and agglomeration. An endotracheal administration device was used to aerosolize the suspension. This mode of delivery was evaluated at different temozolomide concentrations and was optimized for the uniformity of delivered dose, the droplet size distribution and the distribution of droplets in vivo. Of the particles in the stabilized suspension, 79% were compatible with the human respirable size range... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3221375 Mon, 25 Jan 2010 00:00:00 +0100 3221375 http://www.medworm.com/index.php?rid=3208749&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%3D20096354%26dopt%3DAbstract The objectives of the study were (i) to investigate the effect of experimental parameters on the iontophoretic transport of granisetron, (ii) to identify the relative contributions of electromigration (EM) and electroosmosis (EO), (iii) to determine the feasibility of delivering therapeutic amounts of drug for the treatment of chemotherapy-induced nausea and vomiting and (iv) to test the in vitro results in a simple animal model in vivo. Preliminary in vitro studies using aqueous granisetron formulations investigating the effect of drug concentration (5, 10, 20 and 40mM) and current density (0.1, 0.2, 0.3mA.cm(-2)) were performed using porcine ear skin. As expected, cumulative delivery in vitro at the 20 and 40mM concentrations was significantly greater than that at 5 and 10mM, which were ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3208749 Tue, 19 Jan 2010 00:00:00 +0100 3208749 http://www.medworm.com/index.php?rid=3201968&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%3D20093180%26dopt%3DAbstract CONCLUSIONS: Although this study shows a possible association of polymorphisms of RAAS genes with the risk of non-control of HT in ACEI-treated patients and indicates the importance of all this system's components in regulating HT, it needs to be replicated in other data sources. PMID: 20093180 [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=3201968 Mon, 18 Jan 2010 00:00:00 +0100 3201968 http://www.medworm.com/index.php?rid=3201967&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%3D20093181%26dopt%3DAbstract Authors: Wang T, Wang N, Hao A, He X, Li T, Deng Y A novel procedure for the preparation of hydrophilic peptide-containing oily formulations involving the freeze-drying of water-in-oil emulsions (FWE) is described. A mixture of an aqueous phase containing insulin and and oil phase containing phosphatidylcholine was emulsified to prepare water-in-oil emulsions, which were subsequently lyophilized. Upon addition of oil, the lyophilates formed a clear oily solution which was considered as an anhydrous reverse micelle (ARM) system since it contained no water but 20-nm insulin nanoparticles, as revealed by dynamic light scattering. The 20-nm insulin nanoparticles, existing in a crystal form, were also contained in the lyophilates, as proved by scanning electron microscopy, small angle X-ray... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3201967 Mon, 18 Jan 2010 00:00:00 +0100 3201967 http://www.medworm.com/index.php?rid=3201966&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%3D20093182%26dopt%3DAbstract Authors: Nadarassan DK, Assi KH, Chrystyn H The aerodynamic characteristics of the dose emitted from a dry powder inhaler (DPI) are inhalation flow dependent but have not been determined for low flows. We have designed novel methodology to measure these at <28.3 l min(-1). The original Andersen Cascade Impactor (ACI) designed for use at 60 l min(-1) was adapted to include a mixing inlet (MIXINLET) which allows inhalation flows through the DPI from 5 to 60 l min(-1). The mean fine particle dose (FPD) from a formoterol Turbuhaler using the MIXINLET method at 10, 20, 28.3, 40 and 60 l min(-1) was 0.55, 1.39, 1.80, 2.88 and 5.86mug and the mass median aerodynamic diameter (MMAD) was 6.6, 6.0, 5.4, 5.1 and 2.8mum. Similarly, the FPD using the ACI method was 0.13, 0.69, 1.50, 2.48 and 5.4... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3201966 Mon, 18 Jan 2010 00:00:00 +0100 3201966 http://www.medworm.com/index.php?rid=3201965&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%3D20093183%26dopt%3DAbstract This study demonstrates that PDE5 inhibition attenuates the oxidant burden and the inflammatory and remodeling effects of CSE in human HPAEC which may contribute to the therapeutic value of PDE5 inhibitors for pulmonary disorders coursing with endothelial dysfunction. PMID: 20093183 [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=3201965 Mon, 18 Jan 2010 00:00:00 +0100 3201965 http://www.medworm.com/index.php?rid=3201964&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%3D20093184%26dopt%3DAbstract Authors: Sentellas S, Ramos I, Albertí J, Salvà M, Antón F, Miralpeix M, Beleta J, Gavaldà A Aclidinium bromide is a novel, long-acting inhaled muscarinic antagonist drug in Phase III clinical trials for chronic obstructive pulmonary disease (COPD). The aims of this study were to evaluate the in vitro stability of the ester drug aclidinium in plasma from various species, and the in vitro and in vivo pharmacological activity of its hydrolysis metabolites. Following incubation of aclidinium in pooled samples of human, rat, guinea pig or dog plasma, the rate of hydrolysis was quantified by reversed phase ultra performance liquid chromatography and mass spectrometry. Tiotropium and ipratropium were used as comparators. The in vitro biochemical profile of the hydrolysis ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3201964 Mon, 18 Jan 2010 00:00:00 +0100 3201964 http://www.medworm.com/index.php?rid=3201963&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%3D20093185%26dopt%3DAbstract Authors: Kaiser M, Azeredo FJ, Uchôa FD, Beraldo HD, Costa TD The study aimed to investigate the pharmacokinetics and tissue distribution of the benzaldehyde semicarbazone (BS) a potential antiepileptic drug, administered as a free drug or complexed beta-cyclodextrin (BS/beta-CD). Free BS and BS/beta-CD were administered to male Wistar rats as a 10mg/kg intravenous bolus dose. For the oral route, 50mg/kg and 100mg/kg doses of the free drug and 50mg/kg of the complex were administrated and plasma concentrations were determinated by a validated HPLC-UV method. Individual profiles were evaluated by non-compartmental and compartmental analysis using Excel((R)) and Scientist((R)), respectively. Free BS plasma protein binding was 34+/-5%. A one-compartmental model adequately described a... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3201963 Mon, 18 Jan 2010 00:00:00 +0100 3201963 http://www.medworm.com/index.php?rid=3201962&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%3D20093186%26dopt%3DAbstract This study aims to make a 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD) solubilized itraconazole (ITZ) solution (i.e., HPbetaCD-ITZ) suitable for pulmonary delivery by nebulization, and compare pharmacokinetics of inhaled nebulized aerosols of HPbetaCD-ITZ versus a colloidal dispersion of ITZ nanoparticulate formulation (i.e., URF-ITZ). Solid state characterizations of lyophilized HPbetaCD-ITZ by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS) indicated the formation of dynamic inclusion complexes between ITZ and HPbetaCD. Nebulized aerosols of both HPbetaCD-ITZ and colloidal dispersion of URF-ITZ were confirmed suitable for deep lung delivery. Single doses of the nebulized aerosols (equivalent to 5.3mg ITZ/m... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3201962 Mon, 18 Jan 2010 00:00:00 +0100 3201962 http://www.medworm.com/index.php?rid=3167220&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%3D20060467%26dopt%3DAbstract Authors: Wang Y, Zuo Z, Chen X, Tomlinson B, Chow MS The purpose of the present work was to provide theoretical and experimental support in generating an optimal pH (pH(max)) for a representative weak base compound (propranolol), that can lead to enhanced sublingual absorption. Initially equations for pH-solubility and pH-permeability profiles were derived and compared to the profiles obtained experimentally. Excellent correlation (R(2)=0.999) of solubility profiles was obtained using non-linear regression, and the permeability profiles further predicted that at certain pH (pH(max)), optimal mucosal permeation could be achieved. Subsequently, in a pharmacokinetics study, a buffered sublingual propranolol tablet, designed to achieve its pH(max) (when dissolved in saliva), were compared ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3167220 Thu, 07 Jan 2010 00:00:00 +0100 3167220 http://www.medworm.com/index.php?rid=3167219&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%3D20060468%26dopt%3DAbstract We report on encapsulation of cyanine IR-768 in oil-in-water (o/w) microemulsion, i.e. fabrication of templated polymeric nanocapsules as effective nanocarriers for a new generation of photodynamic agents suitable for photodynamic therapy (PDT). Discussed here are nanocapsule imaging, their in vitro biological evaluation, cyanine encapsulation potential, and the cellular localization of cyanine IR-768 delivered in the nanocapsules to MCF-7 cancer cells. Oil-cored poly(n-butyl cyanoacrylate) (PBCA) nanocapsules were prepared by interfacial polymerization in o/w microemulsions formed by the nonionics Tween 80 (polysorbate 80, polyoxyethylene 20 sorbitan monooleate), and Brij 96 (polyoxyethylene 10 oleyl ether). Iso-propyl myristate (IPM), etyl oleate (EOl), iso-octane (IO), and oleic acid (O... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3167219 Wed, 06 Jan 2010 00:00:00 +0100 3167219 http://www.medworm.com/index.php?rid=3156822&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%3D20056146%26dopt%3DAbstract We present an artificial neural network for modelling human hepatocyte intrinsic clearances (CL(int)) based only on calculated molecular descriptors. In vitro CL(int) data obtained in human hepatocytes suspensions was divided into a train group of 71 drugs for network optimization and a test group of another 18 drugs for early-stop and internal validation resulting in correlations of 0.953 and 0.804 for the train and test group respectively. The model applicability was tested with 112 drugs by comparing the in silico predicted CL(int) with the in vivo Cl(int) estimated by the "well-stirred" model based on the in vivo hepatic clearance (Cl(H)). Acceptable correlations were observed with r values of 0.508 and 63% of drugs within a 10-fold difference when considering blood binding in acidic d... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3156822 Mon, 04 Jan 2010 00:00:00 +0100 3156822 http://www.medworm.com/index.php?rid=3143256&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%3D20045051%26dopt%3DAbstract In conclusion, the results demonstrate the for first time that, in solid-state, n-1 cleavage occurs in parallel to n+1 cleavage at aspartic acid residues and not consecutively. PMID: 20045051 [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=3143256 Tue, 29 Dec 2009 00:00:00 +0100 3143256 http://www.medworm.com/index.php?rid=3133846&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%3D20038453%26dopt%3DAbstract Authors: Kawabata Y, Yamamoto K, Debari K, Onoue S, Yamada S Tranilast (TL) is an anti-allergic agent and widely used in the clinical treatment of bronchial asthma, atopic rhinitis, atopic dermatitis and keloids. However, therapeutic potential of TL could be partly limited because of its poor solubility, bioavailability, and photostability. To overcome these drawbacks, crystalline solid dispersion of TL (CSD/TL) was prepared by wet-milling technique with aim of improving physicochemical and pharmacokinetic properties. Physicochemical properties of the formulations prepared were characterized by laser diffraction and dynamic light scattering for particle size analysis, scanning electron microscope for morphological analysis, and powder X-ray diffraction and differential scanning calorim... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3133846 Fri, 25 Dec 2009 00:00:00 +0100 3133846 http://www.medworm.com/index.php?rid=3126970&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%3D20036738%26dopt%3DAbstract Authors: Pallmann T, Jonas U, Wagner M, Thevis M, Kaeferstein H, Rothschild MA, Bender K The three hydroxybenzodiazepines oxazepam, temazepam, and lorazepam used for their anxiolytic, sedative, and anticonvulsant properties are metabolized by glucuronidation, which is the predominant pathway in the clearance mechanism of exogenous and endogenous substances during phase II metabolism. The aim of this study was the synthesis of benzodiazepine-O-glucuronides as analytical reference substances. All benzodiazepines are prescribed clinically as racemic formulations. The resulting conjugates from the coupling reactions with glucuronic acid are epimeric pairs of glucuronides. Due to the importance of stereochemical factors in drug disposition it is necessary to separate the diastereomeric form... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3126970 Thu, 24 Dec 2009 00:00:00 +0100 3126970 http://www.medworm.com/index.php?rid=3126969&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%3D20036739%26dopt%3DAbstract Authors: Ishiguro T, Hirayama F, Iohara D, Arima H, Uekama K Effects of cyclodextrins on crystallization of chlopropamide and the polymorphic transition mechanism of the drug in aqueous solution were investigated. In the presence of 2-hydroxybutyl-beta-cyclodextrin, chlopropamide was exclusively crystallized to metastable Form II and III polymorphs, whereas it was crystallized to stable Form A in the absence of the beta-cyclodextrin at 4 (o)C. The crystallization to metastable Form II or III polymorph was dependent upon 2-hydroxybutyl-beta-cyclodextrin concentrations employed, i.e. crystallization to Form III at a lower concentration (0.5mM), whereas to Form II in a higher concentration (5mM). At an intermediate concentration (2mM), the least stable Form II crystal was initially precip... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3126969 Thu, 24 Dec 2009 00:00:00 +0100 3126969 http://www.medworm.com/index.php?rid=3126973&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%3D20035863%26dopt%3DAbstract Authors: Vellonen KS, Häkli M, Merezhinskaya N, Tervo T, Honkakoski P, Urtti A Monocarboxylate transporters (MCTs) are transmembrane proteins capable of transferring lactate and other endogenous and exogenous monocarboxylates across the cell membrane. The aim of the present study was to assess the expression and transporter role of human MCT1, MCT3 and MCT4 in the corneal epithelium, corneal epithelial cell lines (primary HCEpiC and immortalized HCE cells) and isolated rabbit corneas. MCT1 and MCT4 were expressed in the human corneal epithelium and the cell lines at mRNA and protein levels. Cellular uptake studies showed saturable and pH-dependent L-lactic acid transport, which was inhibited by various monocarboxylates like diclofenac and flurbiprofen. The permeability of benzoic ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3126973 Tue, 22 Dec 2009 00:00:00 +0100 3126973 http://www.medworm.com/index.php?rid=3126972&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%3D20035864%26dopt%3DAbstract Authors: Panagopoulos P, Forbes B, Mitchell SC, Steventon GB The aim of this study was to investigate the feasibility of employing S-carboxymethyl-L-cysteine as a treatment of chronic obstructive pulmonary disease in dogs. To this end the pharmacokinetic parameters of orally administered S-carboxymethyl-L-cysteine were determined in the dog, cow and sheep. Six healthy beagle dogs, six endogenous Greek sheep and four Holstein Fresian calves were orally dosed with 10mg/kg body weight of S-carboxymethyl-L-cysteine. No significant differences in T(max) and T(1/2) were reported between the species. However, significantly higher AUC((0-Last)), 21.56+/-6.67mug hr ml(-1) and AUC(0-infinity), 21.63+/-6.68mug hr ml(-1) were seen in the dogs compared to the sheep and calves. The calculated V(D) w... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3126972 Tue, 22 Dec 2009 00:00:00 +0100 3126972 http://www.medworm.com/index.php?rid=3126971&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%3D20035865%26dopt%3DAbstract Authors: Nepal PR, Han HK, Choi HK Coenzyme Q(10) (CoQ(10)) was formulated into self-nanoemulsifying drug delivery systems (SNEDDS) to overcome low bioavailability attributed to hydrophobic nature of the drug. Screening of oil phase, surfactants and co-surfactants were performed to select Witepsol((R)) H35, Solutol((R)) HS15 and Lauroglycol((R)) FCC respectively. Ternary phase diagrams were drawn to identify nanoemulsifying region followed by optimization of SNEDDS formulation. The optimized formulation, CoQ(10), Witepsol((R)) H35, Solutol((R)) HS15 and Lauroglycol((R)) FCC in the weight ratio of 1:0.7:4:2 respectively, emulsified readily at 37(o)C with mean emulsion droplet size of 32.4nm. The stability test of the optimized formulation in pH 1.2 and 6.8 buffers confirmed no pH effect... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3126971 Tue, 22 Dec 2009 00:00:00 +0100 3126971 http://www.medworm.com/index.php?rid=3115850&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%3D20025966%26dopt%3DAbstract CONCLUSION: Prediction of mDDIs involving diltiazem requires consideration of both competitive and time-dependent inhibition in gut and liver by both diltiazem and MA, as well as the complex interplay between the two moieties with respect to mutual inhibition of parent compound and its metabolite. PMID: 20025966 [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=3115850 Tue, 15 Dec 2009 00:00:00 +0100 3115850 http://www.medworm.com/index.php?rid=3115849&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%3D20025967%26dopt%3DAbstract Authors: Breslin D, Sato Y, Karki S The degradation kinetics and reaction product profile of the antitumor agent 1 in aqueous solution was studied. Hydrolysis of the pendant imide ring of 1 is the primary mode of thermal degradation in aqueous solution, and the pH rate profile of 1 has a V-shape indicating that hydrolysis of the imide ring can be catalyzed by either acid or base. Hydrolysis of 1 to the anhydride derivative 3 or the dicarboxylic acid derivative 4 is stepwise and the intermediates 2a and 2b formed by initial hydrolytic attack have been observed under alkaline conditions. An overall mechanism for the hydrolysis of 1 in aqueous solution has been proposed. Extrapolating Arrhenius behavior to the hydrolysis reaction of 1 in aqueous solution maintained at a pH value of 4 sugg... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3115849 Tue, 15 Dec 2009 00:00:00 +0100 3115849 http://www.medworm.com/index.php?rid=3068005&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%3D19961929%26dopt%3DAbstract In conclusion, these results suggested that NLS conjugated doxorubicin loaded NPs could be potentially useful as novel drug delivery system for breast cancer therapy. PMID: 19961929 [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=3068005 Tue, 01 Dec 2009 00:00:00 +0100 3068005 http://www.medworm.com/index.php?rid=3068004&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%3D19961930%26dopt%3DAbstract Authors: Kang HE, Chung HJ, Kim HS, Lee JW, Lee MG It has been reported that both liquiritigenin (LQ) and dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylene dioxybiphenyl-2,2'-dicarboxylate (DDB) have a hepatoprotective effect, and administration of both drugs together shows additive protective effect against acute liver injuries. Therefore, the pharmacokinetic interaction between LQ and DDB in rats was studied. LQ (20 and 50mg/kg for the i.v. and p.o. administration, respectively), DDB (10mg/kg for both i.v. and p.o. administration), and both drugs together were once administered intravenously or orally to rats. After the i.v. administration of both drugs together, the Cl(nr) and AUC of LQ were significantly faster (by 30.5%) and smaller (by 22.5%), respectively, than those of without DDB ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3068004 Tue, 01 Dec 2009 00:00:00 +0100 3068004 http://www.medworm.com/index.php?rid=3068003&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%3D19961931%26dopt%3DAbstract Authors: Sanganwar GP, Sathigari S, Babu RJ, Gupta RB Microparticles of a poorly-water-soluble model drug, nevirapine (NEV) were prepared by supercritical antisolvent (SAS) method and simultaneously deposited on the surface of excipients such as lactose and microcrystalline cellulose in a single step to reduce drug-drug particle aggregation. In the proposed method, termed supercritical antisolvent-drug excipient mixing (SAS-DEM), drug particles were precipitated in supercritical CO(2) vessel containing excipient particles in suspended state. Drug/excipient mixtures were characterized for surface morphology, crystallinity, drug-excipient physicochemical interactions, and molecular state of drug. In addition, the drug content uniformity and dissolution rate were determined. A highly orde... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3068003 Tue, 01 Dec 2009 00:00:00 +0100 3068003 http://www.medworm.com/index.php?rid=3068002&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%3D19961932%26dopt%3DAbstract This study therefore investigated the effect of efavirenz on proguanil disposition. Fifteen healthy volunteers were each given 300mg single oral doses of proguanil alone or with the 9(th) dose of efavirenz (400mg daily for 11 days) in a crossover fashion. Blood samples were collected at pre-determined time intervals and analyzed for proguanil and it major metabolite, cycloguanil, using a validated HPLC method. Co-administration of proguanil and efavirenz resulted in significant increases (p<0.05) in C(max), T(max), AUC(T) and elimination half-life (T((1/2)beta)) of proguanil compared with values for proguanil alone [C(max): 2.55+/-0.24 vs 3.75+/-0.48mg/l; T(max): 2.80+/-0.99 vs 4.80+/-0.99h; AUC(T): 45.58+/-12.75 vs 97.00+/-23.33mg.h/l; T((1/2)beta):16.50+/-4.55 vs 23.24+/-4.08h]. Also,... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3068002 Tue, 01 Dec 2009 00:00:00 +0100 3068002 http://www.medworm.com/index.php?rid=3068001&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%3D19961933%26dopt%3DAbstract Authors: Baek IH, Lee BY, Kang W, Kwon KI Several strategies for overcoming the challenge of establishing bioequivalence (BE) for highly variable drugs (HVDs; drugs having within-subject variability>0.3) have been considered in recent years. Within-subject variability of the area under the curve (AUC(4h)) and peak concentration (C(max)) of doxifluridine in the minimal group (n=24) were 0.444 and 0.491, respectively, meeting the criteria for an HVD. For the large group (n=60), within-subject variability of the AUC(4h) and C(max) were 0.431 and 0.493, respectively. The 90% confidence interval for the AUC(4h) and C(max) of the ratio of the test drug to the reference drug exceeded the acceptable BE limits (0.80-1.25) of the ABE (average bioequivalence), in both the minimal and large gro... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3068001 Tue, 01 Dec 2009 00:00:00 +0100 3068001 http://www.medworm.com/index.php?rid=3059939&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%3D19958830%26dopt%3DAbstract Authors: Preetz C, Hauser A, Hause G, Kramer A, Mäder K Oily core nanocapsules were prepared by sequential addition of positively and negatively charged polyelectrolytes based on a nanoemulsion and transformation thereof into a core-shell structure. The capsules were well characterized by photon correlation spectroscopy, laser diffraction, zeta-potential and transmission electron microscopy and feature an average size of 150nm and a negative surface charge. The aim of the current study was to improve the dispersion stability and mechanic rigidity of the capsule wall by depositing an increasing number of up to five layers. Therefore, atomic force microscopy (AFM) and ultrasonic resonator technology (URT) were applied to investigate the shell of the nanoemulsion, the intermediate an... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3059939 Mon, 30 Nov 2009 00:00:00 +0100 3059939 http://www.medworm.com/index.php?rid=3059938&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%3D19958831%26dopt%3DAbstract Authors: Johnson TJ, Gupta KM, Fabian J, Albright TH, Kiser PF Dual segment polyurethane intravaginal rings (IVRs) were fabricated to enable sustained release of antiretroviral agents dapivirine and tenofovir to prevent the male to female sexual transmission of the human immunodeficiency virus. Due to the contrasting hydrophilicity of the two drugs, dapivirine and tenofovir were separately formulated into polymers with matching hydrophilicity via solvent casting and hot melt extrusion. The resultant drug loaded rods were then joined together to form dual segment IVRs. Compression testing of the IVRs revealed that they are mechanically comparable to the widely accepted NuvaRing((R)) IVR. Physical characterization of the individual IVR segments using wide angle x-ray scattering and diffe... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3059938 Mon, 30 Nov 2009 00:00:00 +0100 3059938 http://www.medworm.com/index.php?rid=3052815&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%3D19948217%26dopt%3DAbstract Design, Synthesis and Anti-Inflammatory Evaluation of PEGylated 4-Methyl & 4, 8-Dimethylcoumarins. Eur J Pharm Sci. 2009 Nov 27; Authors: Pandey MK, Balwani S, Sharma PK, Parmar VS, Ghosh B, Watterson AC Aberrant interaction between the leukocyte and the endothelial cell (EC) resulting from the deregulated expression of cell adhesion molecules (CAMs) on the endothelium results in uncontrolled inflammation leading to various inflammatory disorders. The existing drugs used to modulate the cytokine-induced expression of cell molecules have severe side effects. Therefore, there is an unmet therapeutic need to develop potent and safe drugs to treat inflammatory disorders. In the present study, novel PEGylated and non-PEGylated 4-methyl & 4, 8-dimethylcoumarin derivatives wer... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3052815 Fri, 27 Nov 2009 00:00:00 +0100 3052815 http://www.medworm.com/index.php?rid=3027223&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%3D19932749%26dopt%3DAbstract In conclusion, after oral dosing of NC-IndOEt, IndOEt is converted into IndOH in the intestinal lumen and wall before reaching the blood stream. The complexity of a living system was not predicted by the ex vivo gut sac model. PMID: 19932749 [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=3027223 Fri, 20 Nov 2009 00:00:00 +0100 3027223 http://www.medworm.com/index.php?rid=3027224&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%3D19932176%26dopt%3DAbstract Authors: Dahlberg C, Millqvist-Fureby A, Schuleit M, Furó I We demonstrate that the ability of drugs to influence the wetting of solid dispersion tablets in unexpected ways. Five model drugs of different water solubility and ability to interact with the involved polymers were incorporated in hydrophilic polymer matrices, made of either hydroxypropyl methylcellulose (HPMC) or polyvinyl pyrrolidone (PVP). Physical mixtures of all combinations of drug and polymer presented surface hydrophobicities, as measured by the equilibrium advancing contact angle of water, which are expected for materials that do not influence the interactions of each other with water. However, the solid dispersions containing HPMC deviated from this regular behaviour and displayed contact angles below the ones... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3027224 Thu, 19 Nov 2009 00:00:00 +0100 3027224 http://www.medworm.com/index.php?rid=3027225&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%3D19931387%26dopt%3DAbstract Authors: Saber A, Strand SP, Ulfendahl M Development of efficient local delivery systems for the auditory organ has an important role in clinical practice for the management of inner ear disorders using pharmacological means. Chitosan, a biodegradable polymer, is a good drug carrier with bioadhesive properties. The aim of this study was to investigate the feasibility of using chitosan to deliver drugs to the inner ear across the round window membrane (RWM).Three structurally different chitosans loaded with a tracer drug, neomycin, were injected into the middle ear cavity of albino guinea pigs (n=35). After 7 days the effect of chitosans and neomycin was compared among the treatment groups. The hearing organ was analysed for hair cell loss and the RWM evaluated in term of thickness. All... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3027225 Tue, 17 Nov 2009 00:00:00 +0100 3027225 http://www.medworm.com/index.php?rid=3004636&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%3D19913612%26dopt%3DAbstract Authors: Kadiyala I, Loo Y, Roy K, Rice J, Leong KW Oral vaccination is one of the most promising applications of polymeric nanoparticles. Using two different in vitro cellular models to partially reproduce the characteristics of intestinal enterocytes and M-cells, this study demonstrates that nanoparticle transport through the M-cell co-culture model is 5 fold that of the intestinal epithelial monolayer, with at least 80% of the chitosan-DNA nanoparticles uptaken in the first 30minutes. Among the properties of nanoparticles studied, ligand decoration has the most dramatic effect on the transcytosis rate: transferrin modification enhances transport through both models by 3-5 fold. The stability of the nanoparticles also affects transport kinetics. Factors which de-stabilize the nanopar... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=3004636 Wed, 11 Nov 2009 00:00:00 +0100 3004636 http://www.medworm.com/index.php?rid=2996312&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%3D19903526%26dopt%3DAbstract In conclusion, our results argue against the model that deformable vesicles would carry hydrophilic drugs across the skin and act as a sustained release system in deep tissues. PMID: 19903526 [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=2996312 Sat, 07 Nov 2009 00:00:00 +0100 2996312 http://www.medworm.com/index.php?rid=2996311&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%3D19903527%26dopt%3DAbstract Authors: Chen RN, Ho HO, Yu CY, Sheu MT The aim of this study was to develop an optimal gastroretentive drug delivery system (GRDDS) for administering Losartan. Additionally, the influence of optimized GRDDS on the bioavailability of Losartan and the formation extent of active metabolite E3174 by CYP2C9 polymorphism was investigated. Swellable and floatable GRDDS tablets combining hydroxyethylcellulose (HEC), sodium carboxymethylcellulose (NaCMC), and sodium bicarbonate were prepared at various compression pressures for evaluating swelling characteristics and floating capacity. Then Losartan was incorporated into optimized formulations for in vitro and in vivo characterizations. An appropriate ratio of HEC to NaCMC, addition of sodium bicarbonate, and compression at lower pressures res... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2996311 Sat, 07 Nov 2009 00:00:00 +0100 2996311 http://www.medworm.com/index.php?rid=2980821&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%3D19900541%26dopt%3DAbstract CONCLUSIONS: A higher transfer rate of metformin was detected in fetal-to-maternal than maternal-to-fetal direction, but a similar difference was observed with antipyrine. Inhibition of OCTs did not have a significant effect on the placental transfer of metformin. Although the existence of other active transporting systems cannot be ruled out, the influence of OCT-dependent active transport system on the placental pharmacokinetics of metformin is unlikely significant. PMID: 19900541 [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=2980821 Fri, 06 Nov 2009 00:00:00 +0100 2980821 http://www.medworm.com/index.php?rid=2980819&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%3D19900542%26dopt%3DAbstract In conclusion, gaboxadol acts as a substrate for hPAT1 and is a substrate of rOat1. In rats, 5-HTP decreased the initial absorption rate and increased AUC of gaboxadol. 5-HTP thus had a significant impact on the pharmacokinetic profile of gaboxadol. PMID: 19900542 [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=2980819 Fri, 06 Nov 2009 00:00:00 +0100 2980819 http://www.medworm.com/index.php?rid=2980822&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%3D19897032%26dopt%3DAbstract Authors: Tsuchiya H, Ueno T, Tanaka T, Matsuura N, Mizogami M Certain anesthetics have been suggested to protect against the pathological states associated with oxidative stress. We compared the antioxidant and membrane activities of propofol (2,6-diisopropylphenol) and its related compounds to address the structure-activity relationship especially in a lipid membrane phase. They were studied for the effects on 1,1-diphenyl-2-picrylhydrazyl radicals, nitro blue tetrazolium reduction by superoxide anions and membrane lipid peroxidation by peroxynitrite, and also for the induced changes in membrane fluidity of liposomes. 2-Isopropylphenols scavenged free radicals with the potency being propofol>2,5-diisopropylphenol>2-isopropylphenol>2,4-diisopropylphenol, but not 3- and 4-isopr... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2980822 Thu, 05 Nov 2009 00:00:00 +0100 2980822 http://www.medworm.com/index.php?rid=2980823&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%3D19895885%26dopt%3DAbstract In conclusion, by promoting osteogenic development of hMSCs in vitro, this newly designed controlled release system opens a new door to bone reparation and regeneration. PMID: 19895885 [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=2980823 Tue, 03 Nov 2009 00:00:00 +0100 2980823 http://www.medworm.com/index.php?rid=2955519&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%3D19879945%26dopt%3DAbstract Authors: Schoubben A, Blasi P, Giovagnoli S, Ricci M, Rossi C The aim of the work was to produce capreomycin dry powder and capreomycin loaded PLGA microparticles intended for tuberculosis inhalation therapy, using simple and scalable methods. Capreomycin physico-chemical characteristics have been modified by hydrophobic ion pairing with sodium oleate. The powder suspension was processed by high pressure homogenization and spray-dried. Spray-drying was also used to prepare capreomycin oleate (CO) loaded PLGA microparticles. CO powder was suspended in the organic phase containing PLGA and the suspension was spray-dried. Particle dimensions were determined using photon correlation spectroscopy and Accusizer C770. Morphology was investigated by scanning electron microscopy (SEM) and capre... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2955519 Thu, 29 Oct 2009 00:00:00 +0100 2955519 http://www.medworm.com/index.php?rid=2944818&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%3D19874890%26dopt%3DAbstract Authors: Rajesh G, Harshala S, Dhananjay G, Jadhav A, Vikram G Angiogenesis is a key process needed for the growth and survival of solid tumors. Anti-angiogenesis may arrest the tumor growth and keep check on cancer metastasis. Developing antiangiogenic agents has remained a significant hope in the mainstream of anticancer research. The free radical implications in the initiation of cancers are well established. In the present studies, simple flavone and flavones with hydroxyl substitution in 'A' and 'C' ring at 3, 5, 6, and 7 were studied for antiangiogenic activities using Chorioallantoic Membrane (CAM) model and kinetics of DPPH (2, 2-diphenyl-1-picryl hydrazine) and superoxide anion radical (SOR) scavenging activities. The docking of selected flavones with specific angiogenic targe... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2944818 Mon, 26 Oct 2009 00:00:00 +0100 2944818 http://www.medworm.com/index.php?rid=2944817&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%3D19874891%26dopt%3DAbstract Authors: Kuhli M, Weiss M, Steckel H An in-line sampling system with dilution units for aqueous droplet aerosols from single dose inhalers (Berodual Respimat((R)), Boehringer Ingelheim Pharma GmbH & Co. KG, Germany) for an optical particle counter is described. The device has been designed to interface with a white light aerosol spectrometer (welas((R)) digital 2100, Palas((R)) GmbH, Germany) that allows the time-resolved measurement of highly concentrated aerosols. Performance of the sampling system with regard to the measured particle size distribution (PSD) is compared to Next Generation Impactor (NGI) and to laser diffraction measurements (Sympatec Inhaler and open bench). Optimal settings of the sampling system lead to PSDs that correspond well to those measured by the evapora... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2944817 Mon, 26 Oct 2009 00:00:00 +0100 2944817 http://www.medworm.com/index.php?rid=2931495&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%3D19854270%26dopt%3DAbstract Authors: Khier S, Deleuze-Masquefa C, Moarbess G, Gattacceca F, Margout D, Solassol I, Cooper JF, Pinguet F, Bonnet PA, Bressolle FM In spite of the development of new anticancer drugs by the pharmaceutical industry, melanoma and T lymphomas are diseases for which medical advances remain limited. Thus, there was an urgent need of new therapeutics with an original mechanism of action. Since several years, our group develops quinoxalinic compounds. In this paper, the first preclinical results concerning one lead compound, EAPB0203, are presented. This compound exhibits in vitro cytotoxic activity on A375 and M4Be human melanoma cell lines superior to that of imiquimod and fotemustine. A liquid chromatography-mass spectrometry method was first validated to simultaneously quantify EAPB0203... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2931495 Thu, 22 Oct 2009 00:00:00 +0100 2931495 http://www.medworm.com/index.php?rid=2931492&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%3D19854271%26dopt%3DAbstract Authors: Castillo-Garit JA, Vega MC, Rolon M, Marrero-Ponce Y, Kouznetsov VV, Torres DF, Gómez-Barrio A, Bello AA, Montero A, Torrens F, Pérez-Giménez F Herein we present results of a Quantitative Structure-Activity Relationship (QSAR) studies to classify and design, in a rational way, new antitrypanosomal compounds by using non-stochastic and stochastic bond-based quadratic indices. A data set of 440 organic chemicals, 143 with antitrypanosomal activity and 297 having other clinical uses, is used to develop QSAR models based on Linear Discriminant Analysis (LDA). Non-stochastic model correctly classifies more than 93% and 95% of chemicals in both training and external prediction groups, respectively. On the other hand, the stochastic model shows an accuracy of about the... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2931492 Thu, 22 Oct 2009 00:00:00 +0100 2931492 http://www.medworm.com/index.php?rid=2905616&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%3D19837159%26dopt%3DAbstract In conclusion, age-dependent permeability of intestinal tissue (rather than age-dependent luminal drug solubility) may contribute to altered intestinal drug absorption in older patients compared to young adults. PMID: 19837159 [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=2905616 Wed, 14 Oct 2009 23:00:00 +0100 2905616 http://www.medworm.com/index.php?rid=2902741&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%3D19833200%26dopt%3DAbstract Authors: Dos Santos DF, Nicolete R, Souza PR, Bitencourt CD, Junior RR, Bonato VL, Silva CL, Faccioli LH In the last decades, the incidence of histoplasmosis, a pulmonary fungal disease caused by Histoplasma capsulatum, has increased worldwide. In this context, vaccines for the prevention of this infection or therapies are necessary. Cell-free antigens (CFAgs) from H. capsulatum when administered for murine immunization purposes are able to confer protection and control of the infection, since they activate cellular immunity. However, the most of vaccination procedures need several antigens administrations and immunoadjuvants, which are not approved for use in humans. The aim of this study was to develop and characterize a vaccination approach using biodegradable PLGA microspheres (MS)... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2902741 Sun, 11 Oct 2009 23:00:00 +0100 2902741 http://www.medworm.com/index.php?rid=2902740&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%3D19833201%26dopt%3DAbstract Authors: Bergström CA, Bolin S, Artursson P, Rönn R, Sandström A The purpose of this study was to investigate the intestinal absorption of tripeptide-based compounds intended for treatment of Hepatitis C Virus (HCV) infection. The intestinal permeability of eleven HCV NS3 protease inhibitors (Mw 687-841, ClogD(pH7.4) 1.2-7.3 and 10-13 hydrogen bond donors/acceptors) were measured using Caco-2 cells. Each compound was investigated in the apical to basolateral (a-b) and basolateral to apical (b-a) direction at pH 7.4. For compounds displaying efflux the experiment was repeated in the presence of 1muM GF120918 to investigate possible involvement of P-glycoprotein (Pgp; ABCB1). All compounds displayed intermediate to high permeability. Seven of them showed extensive efflux, ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2902740 Sun, 11 Oct 2009 23:00:00 +0100 2902740 http://www.medworm.com/index.php?rid=2902739&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%3D19833202%26dopt%3DAbstract In conclusion, Ginkgolide B could pass through BBB, especially after ischemia - reperfusion injury of brain, and might be therapeutically effective for ischemia / reperfusion injury of human brain. PMID: 19833202 [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=2902739 Sun, 11 Oct 2009 23:00:00 +0100 2902739 http://www.medworm.com/index.php?rid=2891401&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%3D19819331%26dopt%3DAbstract This study compares the lipid membrane interactions of indacaterol, an ultra long acting beta-2 agonist that is given once a day, to salmeterol, a twice a day beta-2 agonist, in order to elucidate the potential mechanisms leading to their different pharmacology properties. Salmeterol but not indacaterol perturbed dimyristoyl-phosphatidylcholine membranes. While the liposome partitioning of the two compounds was similar, independent of the lipid composition, the membrane affinity of indacaterol was two-fold greater than that of salmeterol when rafts, i.e. detergent-insoluble membrane domains, were used as the partition phase. The observed association kinetics with immobilized liposomes at physiological pH were two times faster for indacaterol than for salmeterol. A new model to explain the ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2891401 Wed, 07 Oct 2009 23:00:00 +0100 2891401 http://www.medworm.com/index.php?rid=2873069&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%3D19804821%26dopt%3DAbstract Authors: Cermak R, Wein S, Wolffram S, Langguth P The influence of the dietary flavonol quercetin on the pharmacokinetics of the HMG-CoA reductase inhibitor simvastatin was investigated in pigs. Simvastatin (0.25mg/kg body weight) was orally administered to 6 pigs either without or with quercetin (10mg/kg). In addition, simvastatin was administered to 3 pigs that had received a diet supplemented with the flavonol over a period of 1 week. Daily quercetin intake was 10mg/kg in these animals. Co ingestion of quercetin with the statin did not alter area under the concentration time curve (AUC(0-->infinity)), time to achieve maximum plasma concentration (t(max)) or half-life (t(1/2)) of simvastatin. However, there was a trend towards a reduction of the maximum plasma concentration (C(max... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2873069 Thu, 01 Oct 2009 23:00:00 +0100 2873069 http://www.medworm.com/index.php?rid=2873068&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%3D19804822%26dopt%3DAbstract This study confirms the interaction of VPA with TPR, which is presumably dependent on VPA dose. PMID: 19804822 [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=2873068 Thu, 01 Oct 2009 23:00:00 +0100 2873068 http://www.medworm.com/index.php?rid=2873067&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%3D19804823%26dopt%3DAbstract In conclusion, the L-dopa nasal delivery system could be used as a good rescue therapy for PD patients who experience symptom fluctuation with oral L-dopa administration. PMID: 19804823 [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=2873067 Thu, 01 Oct 2009 23:00:00 +0100 2873067 http://www.medworm.com/index.php?rid=2873066&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%3D19804824%26dopt%3DAbstract Authors: Schultheiss N, Smit JP, Hanko JA Three crystalline hemi-hydrate, channel solvates (classified as solvates from here on) of finasteride (N-(1,1-di-methylethyl)-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide) have been obtained and fully characterized. The acetone, methyl ethyl ketone (MEK), and toluene solvates of finasteride, described herein, were found to be isostructural and belong as additional members to a family of previously reported finasteride solvates. Vacuum drying at 85 degrees C for one day produced the metastable, anhydrous Form II of finasteride from all three solvated materials. PMID: 19804824 [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=2873066 Thu, 01 Oct 2009 23:00:00 +0100 2873066 http://www.medworm.com/index.php?rid=2873065&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%3D19804825%26dopt%3DAbstract We examined thromboxane A(2) receptor (TP)-mediated transactivation of epidermal growth factor receptor (EGFR) through the shedding of EGFR ligands. A TP agonist U46619 caused the phosphorylation of EGFR in 1321N1 human astrocytoma cells, which was inhibited by an EGFR selective inhibitor AG1478 and by a disintegrin and metalloproteinase (ADAM) inhibitor TAPI-2, indicating TP stimulation caused the EGFR transactivation through the EGFR ligand shedding. Since 1321N1 cells expressed heparin binding-EGF (HB-EGF) mRNA, the mechanism of TP-mediated EGFR transactivation was examined in HEK293 cells expressing alkaline phosphatase-conjugated HB-EGF and TP. U46619 caused the shedding of HB-EGF in a time- and concentration-dependent manner. The TP-mediated shedding was inhibited by a furin inhibito... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2873065 Thu, 01 Oct 2009 23:00:00 +0100 2873065 http://www.medworm.com/index.php?rid=2852132&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%3D19786099%26dopt%3DAbstract We present a mathematical analysis of the basic model underlying target-mediated drug disposition (TMDD) in which a ligand is supplied through an initial bolus or through a constant rate infusion and forms a complex with a receptor (target), which is supplied and removed continuously. Ligand and complex may be eliminated according to first-order processes. We assume that the total receptor pool (free and bound) is constant in time and we give a geometrical description of the evolution of the concentrations of ligand, receptor and receptor-ligand complex which offers a transparent way to compare the full model with simpler models such as the quasi-steady-state (QSS) model, the quasi-equilibrium (QE) model and the empirical Michaelis-Menten (MM) model; we also give precise conditions on the ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2852132 Thu, 24 Sep 2009 23:00:00 +0100 2852132 http://www.medworm.com/index.php?rid=2843103&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%3D19782131%26dopt%3DAbstract Authors: Thi TD, Van Speybroeck M, Barillaro V, Martens J, Annaert P, Augustijns P, Van Humbeeck J, Vermant J, Van den Mooter G In order to gain a better understanding of the reasons of successful self-microemulsifying drug delivery systems (SMEDDS) formulation, ten poorly water-soluble drugs, exhibiting different physicochemical properties, were selected. The solubility of the compounds was determined in various oils (long and medium chain) and surfactants (HLB > 12 and HLB < 10). The best performing excipients were selected for SMEDDS formulation. The droplet size and zeta potential of SMEDDS were measured in the absence and the presence of drug. Media, time and the presence of drug showed little or no influence on droplet size of most systems. Some systems displayed a differen... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2843103 Tue, 22 Sep 2009 23:00:00 +0100 2843103 http://www.medworm.com/index.php?rid=2843102&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%3D19782132%26dopt%3DAbstract Authors: Van Gyseghem E, Stokbroekx S, Armas HN, Dickens J, Vanstockem M, Baert L, Rosier J, Schueller L, Van den Mooter G The interconversion of the ethanolate, hydrate and amorphous form of TMC114 ((3-[(4-amino-benzenesulfonyl)-isobutyl-amino]-1-benzyl-2-hydroxypropyl)-carbamic acid hexahydrofuro-[2,3-b]furan-3-yl ester) in open conditions was characterized. TMC114 hydrate and ethanolate form isostructural channel solvates. The crystal structure of TMC114 was obtained from single crystal X-ray diffraction, confirming that it is a channel solvate. Ethanol and water can exchange with one another. TMC114 ethanolate converts into TMC114 hydrate at moderate or high relative humidity (RH) at 25 degrees C, and it converts back into the ethanolate in ethanol atmosphere. The hydration level o... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2843102 Tue, 22 Sep 2009 23:00:00 +0100 2843102 http://www.medworm.com/index.php?rid=2836462&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%3D19778607%26dopt%3DAbstract Authors: Francesco B, Carmen C, Lucia G, Rotonda L, Immacolata M The enantioselective retention of thirteen -blockers on HPLC stationary phases supporting human serum albumin (HSA) or alpha(1)-acid glycoprotein (AGP) was investigated. Eight beta-blockers were enantiomerically resolved on the AGP column whereas only four beta-blockers were resolved on the HSA column. Moreover, interactions between beta-blockers and AGP were much stronger than those with HSA. Retention values on both HSA and AGP for less retained enantiomers related well with various lipophilicity parameters, with the best relationships found with log(w)(IAM) values obtained on HPLC stationary phases supporting phospholipids, i.e. the so-called Immobilized Artificial Membrane (IAM). Differently from n-octanol lipophilici... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2836462 Sun, 20 Sep 2009 23:00:00 +0100 2836462 http://www.medworm.com/index.php?rid=2815248&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%3D19766186%26dopt%3DAbstract Authors: Adrjanowicz K, Wojnarowska Z, Wlodarczyk P, Kaminski K, Paluch M, Mazgalski J The molecular relaxation in liquid and glassy states of Telmisartan (TEL) has been studied by Broadband Dielectric Spectroscopy (BDS) covering wide temperature and frequency range. Multiple relaxation processes were observed. Besides the primary alpha-relaxation, two secondary relaxations beta and gamma (labelled in order of decreasing time scale) have been reported. Well-separated beta-process observed above and below glass transition temperature T(g), has activation energy E(beta)=81.8kJ/mol and was identified as intermolecular Johari-Goldstein (JG) process. The gamma-relaxation visible in dielectric loss spectra at very low temperatures is most likely non-JG relaxation. The temperature dependence ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2815248 Tue, 15 Sep 2009 23:00:00 +0100 2815248 http://www.medworm.com/index.php?rid=2815252&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%3D19765652%26dopt%3DAbstract Authors: Agüeros M, Ruiz-Gatón L, Vauthier C, Bouchemal K, Espuelas S, Ponchel G, Irache JM The aim of this work was to study the effect of the combination between 2-hydroxypropyl-beta-cyclodextrin (HPCD) and bioadhesive nanoparticles on the encapsulation and intestinal permeability of paclitaxel (PTX). In this context, a solid inclusion complex between PTX and HPCD was prepared by the evaporation method. Then, the complex was incorporated in poly(anhydride) nanoparticles by a solvent displacement method. The resulting nanoparticles, PTX-HPCD NP, displayed a size of about 300nm and a drug loading of about 170mug/mg (500-fold higher than in the absence of HPCD). The effect of these nanoparticles on the permeability of intestinal epithelium was investigated using the Ussing cha... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2815252 Mon, 14 Sep 2009 23:00:00 +0100 2815252 http://www.medworm.com/index.php?rid=2815251&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%3D19765653%26dopt%3DAbstract Authors: Weiss M, Hassna R, Sermsappasuk P, Bednarek T Since it is unclear whether and how propofol affects the alpha(1)-mediated inotropic response, we used a pharmacokinetic-pharmacodynamic modeling approach in isolated rat hearts to analyze the effect of propofol on receptor binding and signal transduction. In Langendorff rat hearts perfused with buffer containing 12.3muM phenylephrine, 1.27nmol doses of [(3)H]-prazosin were infused (over 1min), in the absence and presence of propofol (28muM). Simultaneous analysis of prazosin outflow concentration and inotropic response (left ventricular developed pressure) using an agonist-antagonist interaction model allowed to estimate receptor affinity, as well as the parameters of the operational model of agonism. Propofol significantly (P &lt... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2815251 Mon, 14 Sep 2009 23:00:00 +0100 2815251 http://www.medworm.com/index.php?rid=2815250&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%3D19765654%26dopt%3DAbstract In conclusion, Triple oral hypoglycaemic therapy improves glycemic control, insulin sensitivity, retards diabetic cardiomyopathy and does not increased body weight; decrease more detrimental inflammatory markers, increase interlukin-10 and adiponectin in neonatal streptozotocin induced IRtype2DM Wistar Albino Rats. Triple therapy showed a synergistic effect and was promising in insulin resistance, better in additional cardiovascular risk reduction and those nonresponders to metformin add on glimepiride therapy. PMID: 19765654 [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=2815250 Mon, 14 Sep 2009 23:00:00 +0100 2815250 http://www.medworm.com/index.php?rid=2815249&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%3D19765655%26dopt%3DAbstract Authors: Kummer O, Haschke M, Hammann F, Bodmer M, Bruderer S, Regnault Y, Dingemanse J, Krähenbühl S Macitentan (ACT-064992) is an orally active endothelin receptor antagonist. We first compared the in vitro dissolution characteristics of uncoated and film-coated tablets with hard gelatin capsules containing 10mg ACT-064992. Subsequently, we compared the oral pharmacokinetics of ACT-064992 and its active metabolite ACT-132577 of the coated tablet and the gelatin capsule formulation in 11 male volunteers. The dissolution profile showed a rapid disintegration of all formulations with >90% dissolution of ACT-064992 within 45minutes. The pharmacokinetics of ACT-064992 and its metabolite ACT-132577 were comparable for the two formulations. ACT-064992 revealed a slow absorption... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2815249 Mon, 14 Sep 2009 23:00:00 +0100 2815249 http://www.medworm.com/index.php?rid=2812593&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%3D19761842%26dopt%3DAbstract Authors: Lee DY, Chung HJ, Choi YH, Lee U, Kim SH, Lee I, Lee MG Ipriflavone was reported to be primarily metabolized via hepatic cytochrome P450 (CYP) 1A1/2 and 2C11 in male Sprague-Dawley rats. The protein expression and/or mRNA levels of hepatic CYP1A subfamily and 2C11 was reported to be increased and decreased, respectively, in diabetic rats induced by streptozotocin (DMIS rats). Thus, the pharmacokinetic parameters of ipriflavone and its two metabolites, M1 and M5, were compared after the i.v. (20mg/kg) and p.o. (200mg/kg) administration of ipriflavone to control and DMIS rats. After both i.v. and p.o. administration of ipriflavone to DMIS rats, the AUCs of ipriflavone were significantly smaller (by 31.7% and 34.2% for i.v. and p.o. administration, respectively) than controls. Th... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2812593 Sun, 13 Sep 2009 23:00:00 +0100 2812593 http://www.medworm.com/index.php?rid=2801088&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%3D19748574%26dopt%3DAbstract Authors: Li H, Kiang YH, Jona J Polymorph screening of Compound A, an investigational drug, revealed two anhydrous polymorphs (Forms I and II) and two monohydrates (Forms III and IV) of this pharmaceutical solid. The physiochemical properties of the four forms were characterized by thermal analysis, hot-stage microscopy, equilibrium solubility and intrinsic dissolution rate measurements, and X-ray powder diffraction. Inter-conversion relationship of the four forms was fully elucidated. Thermodynamic stability relationship was inferred from melting data for Form I and Form II and evaluated by van't Hoff plot for Form III and Form IV. Form I and Form III were found to be the more stable anhydrous and hydrate form, respectively. Anhydrous Form I was selected for further pharmaceutical dev... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2801088 Wed, 09 Sep 2009 23:00:00 +0100 2801088 http://www.medworm.com/index.php?rid=2801087&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%3D19748575%26dopt%3DAbstract Authors: Yawata A, Matsuhashi Y, Kato H, Uemura K, Kusano G, Ito J, Chikuma T, Hojo H Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, which has been used as a traditional Chinese medicine due to its anti-inflammatory, analgesic or anti-pyretic action, was examined for inhibition of nucleoside transport and synergistic potentiation of methotrexate cytotoxicity. Cimicifugoside inhibited uptake of uridine, thymidine and adenosine in human leukemia U937 cells with the low nanomolar IC(50) values, but did not affect that of uracil, leucine or 2-deoxyglucose at </=100nM. Cimicifugoside analogs differentially inhibited uridine uptake in the order cimicifugoside > cimicifugenin (aglycon of cimicifugoside) > bugbanoside B > cimicifugenin A, O-methyl cimicifugenin an... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2801087 Wed, 09 Sep 2009 23:00:00 +0100 2801087 http://www.medworm.com/index.php?rid=2801089&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%3D19747542%26dopt%3DAbstract Authors: McAuley WJ, Mader KT, Tetteh J, Lane ME, Hadgraft J Attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy has been used to simultaneously follow the diffusion of model drugs and solvent across polydimethylsiloxane (silicone) membrane. Three model drugs, cyanophenol (CNP), methyl nicotinate (MN) and butyl paraben (BP) were selected to cover a range of lipophilicities. Isostearyl isostearate (ISIS) was chosen as the solvent because its large molecular weight should facilitate observation of whether the drug molecules are able to diffuse through the membrane independently of the solvent. The diffusion of the three drugs and the solvent was successfully described by a Fickian model. The effects of parameters such as the absorption wavelength used to follo... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2801089 Mon, 07 Sep 2009 23:00:00 +0100 2801089 http://www.medworm.com/index.php?rid=2783123&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%3D19737613%26dopt%3DAbstract Authors: Maher S, Kennelly R, Bzik VA, Baird AW, Wang X, Winter D, Brayden DJ The effects of two absorption promoters, (sodium caprate (C(10)) and melittin), on intestinal permeability and viability were measured in intact rat and human colonic epithelia mounted in Ussing chambers. Apical-side addition of C(10) (10mM) and melittin (10-50muM) rapidly reduced the transepithelial electrical resistance (TEER) and increased the apparent permeability coefficient (Papp) of [(14)C]-mannitol and FITC-dextran-4 kDa (FD4) across colonic mucosae from both species. Effects of C(10) on flux were greater than those of melittin at the concentrations selected. C(10) irreversibly decreased TEER, but the effects of melittin were partially reversible. Enhanced permeability of polar sugars (0.18-70 kDa) in... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2783123 Fri, 04 Sep 2009 23:00:00 +0100 2783123 http://www.medworm.com/index.php?rid=2778762&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%3D19733657%26dopt%3DAbstract Authors: Javeed A, Ashraf M, Ghafoor A, Mukhtar MM Chemotherapy remains the mainstay of treatment for both early stage as well as metastatic tumors. Paclitaxel (PTX), a novel anticancer drug, is a prominent taxane which is active against a broad range of tumors that are generally considered to be refractory to conventional chemotherapy, with benefits gained in terms of overall survival and disease-free survival. PTX is initially characterized as a mitotic inhibitor, and its anti-neoplastic effect is derived from binding to tubulin and excessive microtubule stabilization. Interestingly, drugs traditionally used for tumor cytoreduction, can exert both positive and negative effects on the host's immune system. PTX also exerts effects on the immune system and displays immunomodulatory trai... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2778762 Wed, 02 Sep 2009 23:00:00 +0100 2778762 http://www.medworm.com/index.php?rid=2778761&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%3D19733658%26dopt%3DAbstract In this study, for the first time, TMC/MCC complex nanoparticles as a delivery system and as an adjuvant were developed and evaluated to obtain systemic and mucosal immune responses against nasally administered tetanus toxoid (TT). Nanoparticles were developed by complexation between the oppositely charged chitosan derivatives, N-trimethyl chitosan (TMC, polycationic) and mono-N-carboxymethyl chitosan (MCC, polyampholytic) without using any crosslinker for mucosal vaccination. The cellular viability was found to be higher with TMC/MCC complex compared to that of MCC and TMC alone. Size, zeta-potential and morphology of the nanoparticles were investigated as a function of preparation method. Nanoparticles with high loading efficacy (95%) and positively charged surface were obtained with an ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2778761 Wed, 02 Sep 2009 23:00:00 +0100 2778761 http://www.medworm.com/index.php?rid=2778760&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%3D19733659%26dopt%3DAbstract Authors: Chan LS, Yue PY, Mak NK, Wong RN MicroRNAs (miRNAs) are small non-coding RNAs that act as post-transcriptional gene modulators. Ginsenoside-Rg1, one of the active components of ginseng, has been confirmed as an angiogenesis inducer. Using miRNA microarray analysis, a total of 17 (including miR-214) and 5 miRNAs were found to be down- or up-regulated by Rg1 in human umbilical vein endothelial cells (HUVEC), respectively. Since miR-214 is closely related to endothelial nitric oxide synthase (eNOS) and hence angiogenesis; its expression was further validated by qRT-PCR. We also investigated the role of miR-214 on eNOS expression and in tubulogenesis and motility of HUVEC by transfection of specific miRNA inhibitor or precursor. Our results suggested that Rg1 can down-regulate miR... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2778760 Wed, 02 Sep 2009 23:00:00 +0100 2778760 http://www.medworm.com/index.php?rid=2778764&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%3D19732829%26dopt%3DAbstract This study investigated the relationship between surface energy of micronized lactose, coarse lactose and salmeterol xinafoate and dispersibility from a mixture after storage at 75% RH. Surface energies, dispersibility, morphology, and presence of amorphous domains were determined by Inverse Gas Chromatography, Twin Stage Impinger, Scanning Electron Microscope and Dynamic Vapour Sorption, respectively. The fine particle fraction of mixture decreased significantly in four weeks (P<0.05), reaching a static level in three months. Amorphous content was not detected in the micronized lactose, coarse lactose and salmeterol xinafoate. After conditioning stored samples at 75% RH for two hours, dispersive surface energy of both micronized and coarse lactose significantly decreased (P<0.05), w... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2778764 Mon, 31 Aug 2009 23:00:00 +0100 2778764 http://www.medworm.com/index.php?rid=2778763&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%3D19732830%26dopt%3DAbstract Authors: Cha EJ, Kim JE, Ahn CH Methoxy poly(ethylene glycol)-block-oligo(L-aspartic acid)-block-poly(varepsilon-caprolactone) with four aspartic acid groups was synthesized with a molecular weight and M(w)/M(n) of 8,930 and 1.22. Polymeric micelles were formed by dialysis and stabilized by electrostatic interactions between the carboxylic acid groups and calcium cations. The critical micelle concentration of mPEG-Asp-PCL was determined to be 0.078mg/mL. At 0.02mg/mL, the dissociation of micelles without ionic stabilization formed an opaque, phase-separated solution, while the stabilized micelles under the same conditions showed structural stability through ionic stabilization. The paclitaxel-loading and efficiency were 8.7 % and 47.6 %, respectively, and the drug loading increased the... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2778763 Mon, 31 Aug 2009 23:00:00 +0100 2778763 http://www.medworm.com/index.php?rid=2752963&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%3D19720145%26dopt%3DAbstract In this study, the ability of XN to inhibit bovine viral diarrhea virus (BVDV), a surrogate model of hepatitis C virus (HCV), was investigated. The antiviral activity of XN was compared with that of ribavirin (RBV) and interferon (IFN)-alpha. The results showed that XN could inhibit BVDV induced cytopathic effects (CPE). At 1000 TCID(50) and 100 TCID(50), the values of 50% effective concentration (EC(50)) were 3.24+/-0.02mg/l and 2.77+/-0.19mg/l, respectively, and the therapeutic indices were >7.72 and >9.03, respectively. XN inhibited BVDV E2 expression and viral RNA levels in a dose-dependent manner. At 6.25mg/l, XN decreased the viral RNA from released virus by 3.83 log10 at 1000 TCID(50) and to an undetectable level at 100 TCID(50,) and decreased the viral RNA level in whole cell... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2752963 Thu, 27 Aug 2009 23:00:00 +0100 2752963 http://www.medworm.com/index.php?rid=2752964&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%3D19716414%26dopt%3DAbstract This study has investigated the utility and potential advantages of an artificial intelligence technology- neurofuzzy logic- as a modeling tool to study direct compression formulations. The modeling performance was compare with traditional statistical analysis. From results it can be stated that the normalized error obtained from neurofuzzy logic was lower. Compared to the multiple regression analysis neurofuzzy logic showed higher accuracy in prediction for the five outputs studied. Rule sets generated by neurofuzzy logic are completely in agreement with the findings based on statistical analysis and advantageously generate understandable and reusable knowledge. Neurofuzzy logic is easy and rapid to apply and outcomes provided knowledge not revealed via statistical analysis. PMID: 197... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2752964 Tue, 25 Aug 2009 23:00:00 +0100 2752964 http://www.medworm.com/index.php?rid=2744440&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%3D19712742%26dopt%3DAbstract Authors: Briones E, Colino CI, Lanao MJ The selectivity of amikacin in macrophages in vitro and its biodistribution in peritoneal macrophages and other tissues were studied in rats using carrier erythrocytes. Amikacin-loaded erythrocytes were prepared using a hypotonic dialysis method. The in vitro uptake of amikacin by peritoneal macrophages was studied using cell monolayers. The in vivo uptake by macrophages and the tissue distribution of amikacin were studied in two groups of rats that received either amikacin in saline solution, or amikacin-loaded erythrocytes. Pharmacokinetic analyses were performed using model-independent methods. The administration of the antibiotic using carrier erythrocytes elicited a higher accumulation in macrophages, both in vitro and in vivo. The tissue ph... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2744440 Sun, 23 Aug 2009 23:00:00 +0100 2744440 http://www.medworm.com/index.php?rid=2725589&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%3D19695327%26dopt%3DAbstract Authors: Boga C, Fiume L, Baglioni M, Bertucci C, Farina C, Kratz F, Manerba M, Naldi M, Di Stefano G In order to improve the efficacy of doxorubicin (DOXO) in the treatment of hepatocellular carcinomas, the drug was conjugated with lactosaminated human albumin (L-HSA), a hepatotropic drug carrier. Conjugation was performed using the (6-maleimidocaproyl)hydrazone derivative of the drug (DOXO-EMCH). The maleimide group of DOXO-EMCH reacts with the aminoacidic residues of the carrier forming stable bonds, whereas the hydrazone bond is rapidly hydrolysed in the acidic endosomal and lysosomal compartments of the cells allowing the intracellular release of DOXO. To identify the amino acids of L-HSA involved in the bond with DOXO-EMCH, in the present study we synthesized this compound with t... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2725589 Sun, 16 Aug 2009 23:00:00 +0100 2725589 http://www.medworm.com/index.php?rid=2716486&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%3D19686846%26dopt%3DAbstract Authors: Van Eerdenbrugh B, Van Speybroeck M, Mols R, Houthoofd K, Martens JA, Froyen L, Van Humbeeck J, Augustijns P, Van Den Mooter G Solid dispersions were successfully prepared by co-spray-drying of TPGS-stabilized itraconazole nanosuspensions with Aerosil((R))200, followed by heat treatment of the powders. The itraconazole/ Aerosil((R))200 weight ratios amounted to 50/50, 30/70, 40/60 and 20/80. The itraconazole content of the powders was close to the expected value, with relative errors between 0.3 and 7.8%. XRPD, SSNMR and DSC evaluation on the powders revealed the formation of amorphous itraconazole and the absence of glassy itraconazole. Dissolution of the powders was enhanced compared to crystalline and glassy itraconazole (a 2-dimensional structured form of itraconazole). Ho... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2716486 Thu, 13 Aug 2009 23:00:00 +0100 2716486 http://www.medworm.com/index.php?rid=2692740&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%3D19666114%26dopt%3DAbstract Authors: Gil EC, Colarte AI, Bataille B, Brouillet F, Caraballo I The aim of this work is to estimate the excipient percolation threshold for a new combined matrix native dextran (DT), serie B110-1-2 (Mw 2x10(6)): HPMC K4M CR: lobenzarit disodium (LBD) system and demonstrate the advantages of this ternary system with respect to previously reported binary dextran:LBD and HPMC:LBD tablets. The formulations studied were prepared with different amount of excipient (DT:HPMC, 4:1wt/wt for all tablets and relative polymer/drug particle size of 4.17) in the range of 10-70% wt/wt. Dissolution studies were carried out using the paddle method (100 r.p.m) and one face water uptake measurements were performed using a modified Enslin apparatus. The Higuchi's models as well as the non-linear regressi... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2692740 Thu, 06 Aug 2009 23:00:00 +0100 2692740 http://www.medworm.com/index.php?rid=2692743&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%3D19664704%26dopt%3DAbstract Authors: Maher S, Wang X, Bzik V, McClean S, Brayden DJ We compared the effectiveness of two absorption promoters, sodium caprate (C(10)) and melittin, in increasing the bioavailability (F) of poorly absorbed paracellular flux markers across the intestinal mucosae of rats in situ, together with examination of their effects on morphology. C(10) (100mM) and melittin (50muM) significantly increased absorption of FITC-dextran-4 kDa (FD4) following jejunal and colonic instillations. F of FD4 following jejunal instillations with C(10) was increased from 0.07% to 2.3%, while it was increased from 0.07% to 0.53% in the presence of melittin. F of FD4 following colonic instillations with C(10) was increased from 1% to 33% while melittin increased it from 1% to 7%. F of FD70 was unchanged in colo... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2692743 Mon, 03 Aug 2009 23:00:00 +0100 2692743 http://www.medworm.com/index.php?rid=2692742&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%3D19664705%26dopt%3DAbstract Authors: Kuntsche J, Koch MH, Fahr A, Bunjes H Cholesteryl nonanoate (CN), myristate (CM), palmitate (CP) and oleate (CO) alone or in combination were evaluated as matrix lipids for the preparation of supercooled smectic nanoparticles with a high stability against recrystallization during storage. The phase behavior of the cholesterol esters in the bulk was studied by polarizing light microscopy, differential scanning calorimetry (DSC) and small angle X-ray scattering (SAXS). Colloidal dispersions with pure and mixed cholesterol ester matrices were prepared by high-pressure melt homogenization and characterized by photon correlation spectroscopy, laser diffraction combined with polarizing intensity differential scattering, DSC and SAXS. The morphology of selected formulations was studi... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2692742 Mon, 03 Aug 2009 23:00:00 +0100 2692742 http://www.medworm.com/index.php?rid=2692741&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%3D19664706%26dopt%3DAbstract Authors: Motoyama K, Kameyama K, Onodera R, Araki N, Hirayama F, Uekama K, Arima H Cyclodextrins (CyDs), which are widely used to increase the solubility of drug in pharmaceutical fields, are known to induce hemolysis and cytotoxicity at high concentrations. However, it is still not unclear whether cell death induced by CyDs is apoptosis or not. Therefore, in the present study, we investigated the effects of various kinds of CyDs on apoptosis in the cells such as NR8383 cells, A549 cells and Jurkat cells. Of various CyDs, methylated CyDs inducted cell death under the present experimental conditions, but hydroxypropylated CyDs and sufobutyl ether-beta-CyD (SBE7-beta-CyD) did not. Of methylated CyDs, 2,6-di-O-methyl-beta-cyclodextrin (DM-beta-CyD) and 2,3,6-tri-O-methyl-beta-cyclodextrin... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2692741 Mon, 03 Aug 2009 23:00:00 +0100 2692741 http://www.medworm.com/index.php?rid=2671583&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%3D19651208%26dopt%3DAbstract Authors: Shah VP, Besançon LJ, Stolk P, Tucker G, Crommelin DJ PMID: 19651208 [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=2671583 Thu, 30 Jul 2009 23:00:00 +0100 2671583 http://www.medworm.com/index.php?rid=2671584&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%3D19646528%26dopt%3DAbstract Authors: Nanjwade BK, Bechra HM, Derkar GK, Manvi FV, Nanjwade VK Dendrimers are new class of polymeric materials. It is generally described as a macromolecule, which is characterized by its extensively branched 3D structure that provides a high degree of surface functionality and versatility. The unique properties associated with these dendrimers such as uniform size, high degree of branching, water solubility, multivalency, well-defined molecular weight and available internal cavities make them attractive for biological and drug-delivery applications. Commercialization of dendrimers is now forthcoming. The present review briefly describes about dendrimer synthesis strategies, types of dendrimers with different functionalities, properties which having crucial importance and their pote... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2671584 Mon, 27 Jul 2009 23:00:00 +0100 2671584 http://www.medworm.com/index.php?rid=2646991&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%3D19632322%26dopt%3DAbstract Authors: Cirstoiu-Hapca A, Buchegger F, Bossy L, Kosinski M, Gurny R, Delie F Paclitaxel (Tx)-loaded anti-HER2 immunonanoparticles (NPs-Tx-HER) were prepared by the covalent coupling of humanized monoclonal anti-HER2 antibodies (trastuzumab, Herceptin((R))) to Tx-loaded poly (DL-lactic acid) nanoparticles (NPs-Tx) for the active targeting of tumor cells that overexpress HER2 receptors. The physico-chemical properties of NPs-Tx-HER were compared to unloaded immunonanoparticles (NPs-HER) to assess the influence of the drug on anti-HER2 coupling to the NP surface. The immunoreactivity of sulfo-MBS activated anti-HER2 mAbs and the in vitro efficacy of NPs-Tx-HER were tested on SKOV-3 ovarian cancer cells that overexpress HER2 antigens. Tx-loaded nanoparticles (NPs-Tx) obtained by a salting... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2646991 Wed, 22 Jul 2009 23:00:00 +0100 2646991 http://www.medworm.com/index.php?rid=2646990&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%3D19632323%26dopt%3DAbstract Authors: Petrović J, Ibrić S, Betz G, Parojčić J, Durić Z The main objective of this study was to demonstrate the possible use of dynamic neural networks to model diclofenac sodium release from polyethylene oxide hydrophilic matrix tablets. High and low molecular weight polymers in the range of 0,9-5x10(6) have been used as matrix forming materials and 12 different formulations were prepared for each polymer. Matrix tablets were made by direct compression method. Fractions of polymer and compression force have been selected as most influential factors on diclofenac sodium release profile. In vitro dissolution profile has been treated as time series using dynamic neural networks. Dynamic networks are expected to be advantageous in the modeling of drug relea... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2646990 Wed, 22 Jul 2009 23:00:00 +0100 2646990 http://www.medworm.com/index.php?rid=2646993&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%3D19631270%26dopt%3DAbstract Authors: de Waard H, Grasmeijer N, Hinrichs WL, Eissens AC, Pfaffenbach PP, Frijlink HW In a previous study we have developed a novel process to produce drug nanocrystals. This process, "controlled crystallization during freeze-drying" has shown to be a successful method to increase the dissolution rate of poorly water soluble drugs [de Waard et al., 2008. J. Control. Release 128, 179]. This process consisted of two steps: a solution of a matrix material (mannitol) in water was mixed with a solution of a drug (fenofibrate) in tertiary butyl-alcohol (TBA). This mixture was frozen and subsequently freeze-dried at relatively high temperature (-25 degrees C). Since the solution of matrix and drug in the water-TBA mixture is thermodynamically unstable, it had to be frozen immediately and fa... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2646993 Mon, 20 Jul 2009 23:00:00 +0100 2646993 http://www.medworm.com/index.php?rid=2622641&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%3D19616094%26dopt%3DAbstract The objective of this study was to use spray drying to prepare mucoadhesive dry powders of the antimigraine drug, zolmitriptan, in combination with the natural polymer, chitosan, for nasal administration. The effect of type, molecular weight, and proportion of chitosan on the powder and particle characteristics was also studied. Solutions containing different proportions of chitosans were prepared and spray dried. The chemical stability and content of the drug were determined by HPLC. The morphology and size range of the microparticles were also determined. Solid state analysis was undertaken using thermal methods (DSC/MDSC and TGA), powder X-ray diffraction (PXRD), and Fourier transform infra-red spectroscopy (FT-IR). The drug release profiles were investigated and the time required to re... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2622641 Tue, 14 Jul 2009 23:00:00 +0100 2622641 http://www.medworm.com/index.php?rid=2622640&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%3D19616095%26dopt%3DAbstract This study tests the hypothesis that pegylated cationic liposomes are a viable carrier for inhalable formulations of low molecular weight heparin, an anionic drug. Cationic liposomal formulations of low molecular weight heparin were prepared by the hydration method using 1,2-dioleoyl-3-trimethylammonium-propane (chloride salt), cholesterol and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethyleneglycol)-2000]. The formulations were characterized for particle size, entrapment efficiency, pulmonary absorption and pharmacological efficacy. For absorption studies, the formulations were administered to anesthetized male Sprague-Dawley rats via the pulmonary route and drug absorption was monitored by measuring plasma anti-factor Xa activity. The pharmacological efficacy of the ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2622640 Tue, 14 Jul 2009 23:00:00 +0100 2622640 http://www.medworm.com/index.php?rid=2622639&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%3D19616096%26dopt%3DAbstract Authors: Ali AM, de Matas M, York P, Rowe RC Variations in pellet filling into hard shell capsules and other cavities are attributed to many factors including fluctuations in pellet size, shape polydispersity, presence of aggregates and electrostatic charge. The influence of pellet aggregation has not previously been investigated, and therefore modelling of the filling behaviour of pellet populations with different levels of twin, triplet and tetrahedral aggregates was evaluated in this study. Pellet/aggregate mixtures were also filled experimentally alongside simulation. The experimental and simulation results for fill weight variability showed that predictions of the trends and values of the percentage coefficient of weight variation (% CV) for mixtures containing twin aggregates up ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2622639 Tue, 14 Jul 2009 23:00:00 +0100 2622639 http://www.medworm.com/index.php?rid=2622638&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%3D19616097%26dopt%3DAbstract Authors: Liu Z, Guo Z, Wang G, Zhang D, He H, Li G, Liu Y, Higgins D, Walsh A, Shanahan-Prendergast L, Lu J The development of novel antiviral drugs is necessary for the prevention and treatment of a potential avian influenza pandemic. The aim of this study was to evaluate the efficacy and safety of a novel statin/caffeine combination against H5N1, H3N2 and H1N1 virus infection in a murine model. In H5N1-, H3N2- and H1N1-infected BALB/c mice, 50mug statin/200mug caffeine effectively ameliorated lung damage and inhibited viral replication and was at least as effective as oseltamivir and ribavirin. The statin/caffeine combination also appeared to be more effective when administered preventatively rather than as treatment. These findings provide justification for further research into thi... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2622638 Tue, 14 Jul 2009 23:00:00 +0100 2622638 http://www.medworm.com/index.php?rid=2532480&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%3D19379811%26dopt%3DAbstract Authors: Kakhi M This paper examines the dissolution apparatus referred to as the flow-through cell from an engineering fluid mechanics viewpoint. The analysis demonstrates that laminar flow predominantly occurs in the standard operation of this apparatus. It is argued that fully turbulent conditions are unlikely. Consequently, the phrases 'open column' and 'packed column' are suggested as technically more accurate terms for its operational characteristics than the conventionally referenced 'turbulent mode' and 'laminar mode'. Examples of flow profiles are given to show that the criterion of a "sinusoidal" input flow profile required by USP is not a sufficiently accurate characterization at the inlet as numerous profiles can be conceived which have the same average flow rate. The ratio... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532480 Sat, 27 Jun 2009 15:59:59 +0100 2532480 http://www.medworm.com/index.php?rid=2532477&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%3D19379812%26dopt%3DAbstract The objective of this work was to investigate the mechanism of release of active pharmaceutical ingredients (APIs) both small molecules (ketoprofen, indomethacin, coumarin-6) and macromolecules (human serum albumin, ovalbumin), from PLGA (50:50) nanoparticulates (400-700nm), having drug loadings less than 10%. The nanoparticulates were prepared by emulsification/solvent evaporation methods and release determined in phosphate buffer pH 7.4 at 37 degrees C. The release profiles exhibited an initial burst release phase, a slower lag phase and a second increased release rate phase. The profiles were consistent with a model in which the first phase of the release reflects diffusion controlled dissolution of drug accessible to the solid/dissolution medium interface and the second phase reflects ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532477 Sat, 27 Jun 2009 15:59:56 +0100 2532477 http://www.medworm.com/index.php?rid=2532474&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%3D19394420%26dopt%3DAbstract Authors: Rodrigues AC, Curi R, Hirata MH, Hirata RD The mechanisms underlying atorvastatin supression of ABCB1 gene expression, at transcriptional and post-transcriptional levels of ABCB1 gene in HepG2 (human hepatocellular carcinoma) cells were investigated. Quantitative real-time PCR was used to measure mRNA levels, as well as to estimate the half-life of ABCB1 mRNA. Western blotting analysis was performed in order to measure protein levels of ABCB1. Electrophoretic mobility shift assay (EMSA) was used to evaluate interactions between protein(s) and ABCB1 promoter region. Exposure to atorvastatin for 24h resulted in a dose-dependent decrease of ABCB1 mRNA and protein levels, which was not abolished by addition of farnesyl or geranylgeranyl pyrophosphate. After removing fetal bovine s... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532474 Sat, 27 Jun 2009 15:59:51 +0100 2532474 http://www.medworm.com/index.php?rid=2532471&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%3D19394421%26dopt%3DAbstract Authors: Graeser KA, Patterson JE, Zeitler JA, Gordon KC, Rades T Poor physical stability is one of the single most important factors limiting the widespread use of the amorphous state in pharmaceutics. The purpose of this study is to move away from the case study approach by investigating thermodynamic and kinetic parameters as potential predictors of physical stability of amorphous drugs for a larger sample set (12 drugs). The relaxation time, fragility index and configurational thermodynamic properties (enthalpy, entropy and Gibbs free energy) were calculated and correlated to the actual stability behaviour, obtained for 12 drugs. Below the glass transition temperature the relaxation time and fragility showed no correlation with the observed physical stability. All drugs were calcul... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532471 Sat, 27 Jun 2009 15:59:46 +0100 2532471 http://www.medworm.com/index.php?rid=2532468&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%3D19406228%26dopt%3DAbstract Authors: Mota FL, Carneiro AP, Queimada AJ, Pinho SP, Macedo EA In this work, pure solvent solubilities of drugs, such as paracetamol, allopurinol, furosemide and budesonide, measured in the temperature range between 298.2-315.2K are presented. The solvents under study were water, ethanol, acetone, ethyl acetate, carbon tetrachloride and n-hexane. Measurements were performed using the shake-flask method for generating the saturated solutions followed by compositional analysis by HPLC. Previous literature values on the solubilities of paracetamol were used to assess the experimental methodology employed in this work. No literature data was found for any of the other drugs studied in this assay. Melting properties of the pure drugs were also determined by differential scanning calorimetr... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532468 Sat, 27 Jun 2009 15:59:43 +0100 2532468 http://www.medworm.com/index.php?rid=2532465&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%3D19406229%26dopt%3DAbstract Authors: Windbergs M, Strachan CJ, Kleinebudde P Different combinations of monoacid triglycerides and polyethylene glycol powders of different molecular weights were successfully extruded below their melting temperatures as a basis for oral dosage forms. The incorporated polyethylene glycols exhibiting different mean molecular weights were compared with respect to their effect on the dissolution rate for a model drug, and a mean molecular weight of 10,000 resulted in the most advantageous characteristics (fastest dissolution). Triglycerides with different fatty acid chain lengths provided additional options for the extrusion temperature which is beneficial for temperature sensitive active pharmaceutical ingredients. To obtain stable extrudates with desirable and reproducible dissolutio... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532465 Sat, 27 Jun 2009 15:59:40 +0100 2532465 http://www.medworm.com/index.php?rid=2532462&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%3D19406230%26dopt%3DAbstract This study employs artificial neural networks (ANNs) to create a model to identify relationships between variables affecting drug nanoprecipitation using microfluidic reactors. The input variables examined were saturation levels of prednisolone, solvent and antisolvent flow rates, microreactor inlet angles and internal diameters, while particle size was the single output. ANNs software was used to analyse a set of data obtained by random selection of the variables. The developed model was then assessed using a separate set of validation data and provided good agreement with the observed results. The antisolvent flow rate was found to have the dominant role on determining final particle size. PMID: 19406230 [PubMed - in process] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532462 Sat, 27 Jun 2009 15:59:38 +0100 2532462 http://www.medworm.com/index.php?rid=2532459&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%3D19406231%26dopt%3DAbstract In conclusion, SLN with small particle size, high EE, and relatively high DL for doxorubicin can be obtained by this method. PMID: 19406231 [PubMed - in process] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532459 Sat, 27 Jun 2009 15:59:35 +0100 2532459 http://www.medworm.com/index.php?rid=2532456&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%3D19409985%26dopt%3DAbstract Authors: Laksmana FL, Hartman Kok PJ, Vromans H, Van der Voort Maarschalk K Prediction of diffusion coefficient of polymer materials is important in the pharmaceutical research and becomes the aim of this paper. This paper bases the prediction method on the estimation of the polymer fractional free volume at different environmental conditions. Focussing on glassy polymers, the free volumes of polymer films were estimated using the model of Vrentas et al. [J.S. Vrentas, J.L. Duda, H.-C. Ling, Antiplasticization and volumetric behavior in glassy polymers, Macromolecules 21 (1988) 1470-1475]. The required data are the moisture sorption and glass transition temperature data, which were measured on various hydroxypropyl methylcellulose (used as a model material) free films at different wate... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532456 Sat, 27 Jun 2009 15:59:32 +0100 2532456 http://www.medworm.com/index.php?rid=2532453&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%3D19428223%26dopt%3DAbstract This study aimed to examine the transporter-mediated drug interaction between fexofenadine and fluvastatin in rats. Compared to the control group given fluvastatin alone, the concurrent use of fexofenadine (10 or 20mg/kg) prior to the oral administration of fluvastatin (5mg/kg) decreased the systemic exposure of fluvastatin by 17-51% in rats. Consequently, the bioavailability of oral fluvastatin was significantly lower (p<0.05) in the presence of fexofenadine compared to that from the control group. Furthermore, the intravenous pharmacokinetics of fluvastatin (2mg/kg) was significantly altered by the pretreatment with fexofenadine (20mg/kg, p.o.). The plasma clearance of fluvastatin was reduced by 44% in the presence of fexofenadine. The effect of fluvastatin on the pharmacokinetics of ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532453 Sat, 27 Jun 2009 15:59:30 +0100 2532453 http://www.medworm.com/index.php?rid=2532408&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%3D19442720%26dopt%3DAbstract In conclusion, PS is potentially useful as a pharmaceutical ingredient to improve the oral bioavailability of coadministered P-gp substrates and substrates for certain CYP isoforms. PMID: 19442720 [PubMed - in process] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532408 Sat, 27 Jun 2009 15:58:51 +0100 2532408 http://www.medworm.com/index.php?rid=2532405&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%3D19442721%26dopt%3DAbstract Authors: Da Costa Martins R, Gamazo C, Irache JM Despite vaccination campaigns, brucellosis is still one of the most common bacterial zoonosis in the world. This work describes the development of a novel formulation strategy to the delivery of the Brucella ovis antigenic extract (HS) into ovine mucosal surfaces. Thus, HS was entrapped in conventional and mannosylated poly(anhydride) nanoparticles by the solvent displacement method, and the resulting nanosystems were gamma-irradiated to accomplish the sterilization required for the ophthalmic administration route. Sterilization, at either 10 kGy or 25 kGy, did not modify the size, morphology and antigen content of the nanoparticles. Similarly, the integrity and antigenicity of the entrapped antigen were not affected by gamma-irradiation... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532405 Sat, 27 Jun 2009 15:58:48 +0100 2532405 http://www.medworm.com/index.php?rid=2532399&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%3D19447177%26dopt%3DAbstract In this study, chemical and enzymatic reactions produced only O-glucuronides of clenbuterol, although on the basis of the chemical structure of the aglycone, both O- and N-glucuronides of clenbuterol could be formed. Differences in the production of diastereomers of clenbuterol glucuronides were observed among liver microsomes from the various animals. Dog and bovine liver microsomes were significantly active, and also stereoselective, each producing only one but a different diastereomer. Liver microsomes from rabbit and rat were also rather actively glucuronidating clenbuterol, but human, pig, and moose liver microsomes produced only minor amounts of glucuronides. Human liver microsomes produced only one clenbuterol glucuronide diastereomer, and the same was true of the human UDP-glucuron... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532399 Sat, 27 Jun 2009 15:58:43 +0100 2532399 http://www.medworm.com/index.php?rid=2532393&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%3D19454316%26dopt%3DAbstract This study aimed to characterize the role of basal transporters of the syncytiotrophoblast, which appear to be yet less studied, in the fetal-to-maternal transfer of saquinavir by use of dually perfused human placentas. A dual perfusion of human placenta was performed to study effect of MK-571 and probenecid, inhibitors of the MRP1 and OATP transporters, expressed in the basal trophoblast membrane, on the transfer of saquinavir. The fetal-to-maternal placental transfer of saquinavir in the control group as measured by TPT(AUC)% (absolute fraction of the dose crossing placenta) was 14.0%, which is 73% less than the transfer of the freely diffusible antipyrine. The two inhibitors, MK-571 and probenecid caused a non-significant (P = 0.34 for ANOVA) reduction of 43% and 24%, respectively, in t... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532393 Sat, 27 Jun 2009 15:58:38 +0100 2532393 http://www.medworm.com/index.php?rid=2532390&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%3D19463948%26dopt%3DAbstract Authors: Nolan LM, Tajber L, McDonald BF, Barham AS, Corrigan OI, Healy AM The aim of this study was to investigate the application of a spray-drying process for the production of nanoporous microparticles (NPMPs) to budesonide, and to characterise the particles produced in terms of their suitability for pulmonary delivery. Budesonide was spray dried with and without ammonium carbonate from ethanol/water or methanol/water solutions. The solid-state characteristics and micromeritic (particle size, density, surface area) properties of spray dried powders were assessed. In vitro deposition studies were performed to assess aerosol performance. The densities of the NPMPs were significantly lower and the surface areas significantly higher than for non-porous spray dried or micronised materia... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532390 Sat, 27 Jun 2009 15:58:36 +0100 2532390 http://www.medworm.com/index.php?rid=2532378&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%3D19491005%26dopt%3DAbstract Authors: Waibel B, Albert C, Holzgrabe U The extent of protein binding is one of the key parameters in both pharmacodynamics and pharmacokinetics. Since a high protein binding prevents the drug to reach the target enzyme or receptor in the organism and the metabolism and excretion of drug, a low protein binding is preferable. Thus, the protein binding has to be considered in the process of drug development. In order to keep the extent of protein binding low it is necessary to know the mechanism of protein-drug interaction. Because NMR methods are able to provide such structural information the purpose of this paper is to compare relaxation and diffusion NMR experiments with a classical protein binding determination method, i.e. ultrafiltration. All of them gave comparable results for t... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532378 Sat, 27 Jun 2009 15:58:25 +0100 2532378 http://www.medworm.com/index.php?rid=2532375&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%3D19491006%26dopt%3DAbstract Authors: Wu ZM, Zhang XG, Zheng C, Li CX, Zhang SM, Dong RN, Yu DM Synthetic hydrogel mimics of the extracellular matrix (ECM) were prepared by cross-linking a thiol-modified chitosan (CS). CS was chemically modified using N-acetyl-l-cysteine (NAC). To minimize interference with biological function, the degree of substitution of thiol groups was kept below 50%. Solution of thiolated CS was prepared in pH 7.4 phosphate buffered saline (PBS) and crosslinked by disulfide bond formation in air. The gelation mainly depended on the content of thiol groups on thiolated CS, concentration of thiolated CS and the molecular weight of CS. Thermogravimetric analysis showed the thermal stabilities of CSS-S hydrogels. Results from SEM observation showed a porous 3D hydrogel structure with pores rangi... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532375 Sat, 27 Jun 2009 15:58:22 +0100 2532375 http://www.medworm.com/index.php?rid=2532372&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%3D19491007%26dopt%3DAbstract The objective of this study was to produce sustained-release matrix tablets by means of injection moulding and to evaluate the influence of matrix composition, process temperature and viscosity grade of ethylcellulose on processability and drug release by means of a statistical design. The matrix tablets were physico-chemically characterized and the drug release mechanism and kinetics were studied. Formulations containing metoprolol tartrate (30%, model drug), ethylcellulose with dibutylsebacate (matrix former and plasticizer) and L-HPC were extruded and subsequently injection moulded into tablets (375mg, 10mm diameter, convex-shaped) at different temperatures (110, 120 and 130 degrees C). Dissolution tests were performed and tablets were characterized by means of DSC, X-ray powder diffrac... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532372 Sat, 27 Jun 2009 15:58:19 +0100 2532372 http://www.medworm.com/index.php?rid=2532369&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%3D19491008%26dopt%3DAbstract Authors: Kamberi M, Nayak S, Myo-Min K, Carter TP, Hancock L, Feder D The major objective of the present study was to develop an accelerated in vitro release method for everolimus/poly(lactic-co-glycolic acid) (PLGA) biodegradable DES that reflects and discriminates between many different sources of variations in the manufacturing process by introducing organic solvents in the release medium. To get further insight into the underlying drug release mechanisms, alongside release studies, the surface changes of the coated stents and the molecular weight changes of the polymer upon immersion in the selected release media were examined by scanning electron microscopy and size exclusion chromatography. The incorporation of acetonitrile in the release medium resulted in an increase in the dru... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532369 Sat, 27 Jun 2009 15:58:16 +0100 2532369 http://www.medworm.com/index.php?rid=2532366&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%3D19491009%26dopt%3DAbstract Authors: Shaikh J, Ankola DD, Beniwal V, Singh D, Kumar MN Curcumin, a derived product from common spice turmeric that is safe and beneficial in several aliments was formulated into biodegradable nanoparticles with a view to improve its oral bioavailability. The curcumin encapsulated nanoparticles prepared by emulsion technique were spherical in shape with particle size of 264nm (polydispersity index 0.31) and 76.9% entrapment at 15% loading. The curcumin encapsulated nanoparticles were able to withstand the International Conference on Harmonisation (ICH) accelerated stability test conditions for refrigerated products for the studied duration of 3 months. X-ray diffraction analysis revealed the amorphous nature of the encapsulated curcumin. The in vitro release was predominantly by dif... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532366 Sat, 27 Jun 2009 15:58:14 +0100 2532366 http://www.medworm.com/index.php?rid=2532364&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%3D19491010%26dopt%3DAbstract Authors: Agüeros M, Areses P, Campanero MA, Salman H, Quincoces G, Peñuelas I, Irache JM This work describes the preparation, characterization and evaluation of the nanoparticles formed by the copolymer of methyl vinyl ether and maleic anhydride (Gantrez) AN) and cyclodextrins, including beta-cyclodextrin (CD) hydroxypropyl-beta-cyclodextrin (HPCD) and 6-monodeoxy-6-monoamino-beta-cyclodextrin (NHCD). The cyclodextrin-poly(anhydride) nanoparticles were prepared by a solvent displacement method and characterized by measuring the size, zeta potential, morphology and composition. For bioadhesion studies, nanoparticles were fluorescently labelled with rhodamine B isothiocianate (RBITC). For in vivo imaging biodistribution studies, (99m)Tc-labelled nanoparticles were used. Nanopar... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532364 Sat, 27 Jun 2009 15:58:09 +0100 2532364 http://www.medworm.com/index.php?rid=2532361&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%3D19491011%26dopt%3DAbstract Authors: Janssens S, Anné M, Rombaut P, Van den Mooter G The presented study aims to explore the feasibility of preparing solid dispersions of the poorly soluble drug, itraconazole, with Kollicoat IR via spray drying, in order to broaden the application window of the polymer. In order to circumvent the need for a common solvent, Kollicoat IR was dissolved in a 50/50 (v/v) water/ethanol mixture and itraconazole was dissolved in a 50/50 (v/v) dichloromethane/ethanol mixture. In a first approach these two solutions were simultaneously spray dried via a spray nozzle with two inlets. In a second approach the two solutions were mixed prior to spray drying and the metastable solution was spray dried via a spray nozzle with a single inlet. This approach was also varied by adding HCl to th... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532361 Sat, 27 Jun 2009 15:58:06 +0100 2532361 http://www.medworm.com/index.php?rid=2532358&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%3D19491012%26dopt%3DAbstract Authors: Cabañas MV, Peña J, Román J, Vallet-Regí M In this work a multifaceted approach to the fabrication of scaffolds is considered, that is, besides the preparation technique, the introduction of substances that may contribute to enhance their final performance, as well as the techniques required to ensure the correct preservation of the so obtained scaffolds are taken into account to tailor the release of vancomycin from beta-tricalcium phosphate (beta-TCP)/agarose scaffolds. These materials were prepared by a shaping technique that allows to obtain pieces at a temperature low enough to simultaneously include active substances susceptible of heat degrading such as vancomycin, the model drug considered in this work. In the first approximation poly(ethylene glyco... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532358 Sat, 27 Jun 2009 15:58:03 +0100 2532358 http://www.medworm.com/index.php?rid=2532357&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%3D19491013%26dopt%3DAbstract Authors: Simões MF, Valente E, Gómez MJ, Anes E, Constantino L Pyrazinamide (PZA) is active against M. tuberculosis and is a first line agent for the treatment of human tuberculosis. PZA is itself a prodrug that requires activation by a pyrazinamidase to form its active metabolite pyrazinoic acid (POA). Since the specificity of cleavage is dependent on a single bacterial enzyme, resistance to PZA is often found in tuberculosis patients. Esters of POA have been proposed in the past as alternatives to PZA however the most promising compounds were rapidly degraded in the presence of serum. In order to obtain compounds that could survive during the transport phase, we synthesized lipophilic ester and amide POA derivatives, studied their activity against M. tuberculosis, their sta... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532357 Sat, 27 Jun 2009 15:57:59 +0100 2532357 http://www.medworm.com/index.php?rid=2532355&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%3D19491014%26dopt%3DAbstract Authors: Moxley R, Day E, Brown K, Mahnke M, Zurini M, Schmitz R, Jones CE, Jarai G The chemokine receptor CCR7 and its ligands CCL19 and CCL21 play an important role in lymphocyte homing and have also been associated with inflammatory, allergic and lung disorders. Cloning of the cynomolgus monkey genes encoding CCR7, CCL19 and CCL21 revealed 93-97% sequence identity of the deduced proteins with their respective human homologs. In chemotaxis assays, B300-19 cells transfected with the cynomolgus (c) CCR7 receptor migrated in response to cCCL19 and cCCL21 in a dose-dependent manner with EC(50) values of 324+/-188nM and 247+/-29nM, respectively. cCCL19 and cCCL21 also elicited calcium responses in stable cell CHO-K1 lines expressing the cCCR7 receptor with EC(50) values of 227+/-4nM and 4... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532355 Sat, 27 Jun 2009 15:57:50 +0100 2532355 http://www.medworm.com/index.php?rid=2532353&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%3D19491015%26dopt%3DAbstract Authors: Wasserman RL, Church JA, Peter HH, Sleasman JW, Melamed I, Stein MR, Bichler J, Intravenous immunoglobulin (IVIg) is used in treating immunodeficiencies and autoimmune or inflammatory disorders. As manufacturing processes and storage can alter IgG molecules, pharmacokinetic assessments are important for new preparations. Thus, we studied pharmacokinetics of IgPro10, a new 10% liquid IVIg product stabilised with l-proline, in patients with common variable immunodeficiency (CVID) and X-linked agammaglobulinaemia (XLA). Patients received IgPro10 for >or=4 months (median dose of 444mg/kg, at 3- or 4-week intervals). Median total IgG serum concentrations increased from 10.2g/l pre-infusion to 23.2g/l at infusion end. Serum IgG concentrations decreased in a biphasic manner; medi... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532353 Sat, 27 Jun 2009 15:57:41 +0100 2532353 http://www.medworm.com/index.php?rid=2532351&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%3D19491016%26dopt%3DAbstract Authors: Roed L, Oulie I, McParland BJ, Skotland T The (99m)Tc complex of NC100692 is being evaluated as a diagnostic agent for the detection of angiogenesis. In the present study, human urine samples from a clinical Phase I study were analysed using reversed-phase liquid chromatography coupled with an ion-trap mass spectrometer (LC-MS) in order to estimate the amount of intact NC100692 and any metabolites excreted in urine following intravenous injection of 150microg (99m)Tc-NC100692. Only intact NC100692 was observed in these urine samples, no metabolites were detected, in contrast to data earlier reported for rat urine where two metabolites and no NC100692 were observed. Within 4-8h after injection, 30+/-6% of the injected NC100692 was excreted in the urine, with the majority (23+/-... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532351 Sat, 27 Jun 2009 15:57:38 +0100 2532351 http://www.medworm.com/index.php?rid=2532349&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%3D19491017%26dopt%3DAbstract Authors: Kendall RA, Alhnan MA, Nilkumhang S, Murdan S, Basit AW Acrylic enteric microparticles for oral drug delivery were prepared by an oil-in-oil emulsion solvent evaporation process. The novel use of sorbitan sesquioleate as a surfactant produced Eudragit L55, L and S (pH thresholds of 5.5, 6 and 7, respectively) microparticles of good morphology (spherical, smooth surfaced), size (<100microm) and size uniformity. The process was efficient (yield approximately 90%) and the encapsulated model drug (prednisolone) was in the amorphous form. The Eudragit L and S microparticles showed excellent pH-responsive drug release in dissolution studies (negligible drug release at pH 1.2; rapid drug release above the polymers' pH thresholds). In contrast, Eudragit L55 particles aggregated in ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532349 Sat, 27 Jun 2009 15:57:36 +0100 2532349 http://www.medworm.com/index.php?rid=2532347&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%3D19491018%26dopt%3DAbstract Authors: D'Arcy DM, Healy AM, Corrigan OI One of the earliest level A in vitro dissolution in vivo absorption correlations (IVIVCs) was established by Levy and co-workers in 1965 using a beaker dissolution apparatus Levy et al., 1965. In the current work, the computational fluid dynamics (CFD) package, Fluent((R)), was used to simulate the hydrodynamics within the Levy beaker apparatus and compare them to those within the paddle and basket apparatuses. In vitro velocity values relevant to in vivo dissolution, presented as apparent gastrointestinal fluid velocity (AGV) values, were calculated. The AGV values were estimated from IVIVCs of immediate release (IR) dosage forms in each apparatus and CFD simulations. The simulations from the Levy apparatus revealed complex hydrodynamics in th... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532347 Sat, 27 Jun 2009 15:57:33 +0100 2532347 http://www.medworm.com/index.php?rid=2532345&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%3D19491019%26dopt%3DAbstract Authors: Song XR, Cai Z, Zheng Y, He G, Cui FY, Gong DQ, Hou SX, Xiong SJ, Lei XJ, Wei YQ Multidrug resistant (MDR) cancer may be treated using combinations of encapsulated cytotoxic drugs and chemosensitizers. To optimize the effectiveness of this combinational approach, poly(d,l-lactide-co-glycolide acid) (PLGA) nanoparticles formulations capable of delivering a cytotoxic drug, vincristine, a chemosensitizer, verapamil, or their combination were prepared via combining O/W emulsion solvent evaporation and salting-out method. Moreover, this work evaluated a number of approaches for the administration of chemosensitizer-cytotoxic drug combinations in a systematic fashion. The results showed that the administration sequence of anticancer drug and chemosensitizer was critical for maximal ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532345 Sat, 27 Jun 2009 15:57:31 +0100 2532345 http://www.medworm.com/index.php?rid=2532343&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%3D19491020%26dopt%3DAbstract In conclusion, carrageenan was able to improve the sustained-release properties of poloxamer 407-based in situ gel, indicating that the combination of carrageenan and poloxamer 407 may find use in the development of vaginal in situ gel drug delivery systems with prolonged local residence and thus better clinical outcome. PMID: 19491020 [PubMed - in process] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532343 Sat, 27 Jun 2009 15:57:28 +0100 2532343 http://www.medworm.com/index.php?rid=2532341&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%3D19491021%26dopt%3DAbstract Authors: Jung SH, Lim DH, Jung SH, Lee JE, Jeong KS, Seong H, Shin BC Lipid nanoparticles (LNPs) as nano-scale drug carriers that can entrap poorly water-soluble drugs such as amphotericin B (AmB) in aqueous solution with high drug entrapment efficiency were developed and their in vitro and in vivo characteristics were investigated. The AmB-entrapping plain, anionic and PEG (polyethylene glycol)-LNPs were prepared by using spontaneous emulsification and solvent evaporation (SESE) method. Mean particle size of the AmB-entrapping LNPs ranged from 72.9 to 159.1nm according to a variation of their lipid composition. The surface of AmB-entrapping PEG (0.2)-LNPs having 84.4+/-6nm of particle size was negatively charged showing -50.4+/-5mV of zeta-potential value. Entrapment efficiency of AmB... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532341 Sat, 27 Jun 2009 15:57:26 +0100 2532341 http://www.medworm.com/index.php?rid=2532338&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%3D19491022%26dopt%3DAbstract Authors: Marosi A, Kovács Z, Béni S, Kökösi J, Noszál B (1)H NMR-pH titrations of cetirizine, the widely used antihistamine and four related compounds were carried out and the related 11 macroscopic protonation constants were determined. The interactivity parameter between the two piperazine amine groups was obtained from two symmetric piperazine derivatives. Combining these two types of datasets, all the 12 microconstants and derived tautomeric constants of cetirizine were calculated. Upon this basis, the conflicting literature data of cetirizine microspeciation were clarified, and the pharmacokinetic absorption-distribution properties could be interpreted. The pH-dependent distribution of the microspecies is provided. PMID: 19491022 [PubMed - in process] ... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532338 Sat, 27 Jun 2009 15:57:22 +0100 2532338 http://www.medworm.com/index.php?rid=2532335&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%3D19491023%26dopt%3DAbstract In this study, the anti-influenza A/WS/33 virus of quercetin 3-rhamnoside (Q3R) from Houttuynia cordata was evaluated using a cytopathic effect (CPE) reduction method, the assay results demonstrated that Q3R possessed strong anti-influenza A/WS/33 virus reducing the formation of a visible CPE. Q3R also did inhibit virus replication in the initial stage of virus infection by indirect interaction with virus particles. However, oseltamivir has relative weaker efficacy compared to Q3R. Therefore, these findings provide important information for the utilization of Q3R for influenza treatment. PMID: 19491023 [PubMed - in process] (Source: European Journal of Pharmaceutical Sciences) European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532335 Sat, 27 Jun 2009 15:57:18 +0100 2532335 http://www.medworm.com/index.php?rid=2532332&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%3D19491024%26dopt%3DAbstract Authors: Podczeck F, Maghetti A, Newton JM The influence of adding two concentrations (5 and 25%) of non-ionic surfactants, one hydrophilic and the other hydrophobic, plus mixtures of equal parts of the two, on the rheological properties of a mixture of equal parts of microcrystalline cellulose and ibuprofen with water has been assessed by capillary rheometry. The mixtures were also used to form pellets by extrusion/spheronization and their in vitro dissolution in simulated intestinal fluid was measured. As with previous rheological studies of these types of pastes, the flow was non-Newtonian (shear thinning). Other rheological parameters were determined in terms of die entry angles, extensional flow and elastic parameters of recoverable shear and compliance. By comparisons with previo... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532332 Sat, 27 Jun 2009 15:57:15 +0100 2532332 http://www.medworm.com/index.php?rid=2532330&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%3D19491025%26dopt%3DAbstract Authors: Moreno D, Zalba S, Colom H, Trocóniz IF, Tros de Ilarduya C, Garrido MJ A biopharmaceutic-pharmacodynamic model is proposed to characterize the antiproliferative effect of controlled release formulations of cisplatin in cancer cell culture. In vitro release profiles from PLGA [poly(d,l-lactide-co-glycolide)] systems were described using a model based on the characterization of two drug release processes: diffusion and matrix degradation. Cytotoxicity data available consisting of the number of survival cells after a continuous exposure to free or encapsulated cisplatin were simultaneously modeled under the Gompertz framework incorporating the drug release model. The release model parameters showed that particle size was inversely related to the diffusion rate. The antiprol... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532330 Sat, 27 Jun 2009 15:57:11 +0100 2532330 http://www.medworm.com/index.php?rid=2532326&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%3D19491026%26dopt%3DAbstract Authors: Kraitzer A, Kloog Y, Zilberman M Farnesylthiosalicylate (FTS) is a new specific nontoxic drug with a mild hydrophobic nature, which acts as a Ras antagonist and can therefore be used for stent applications as well as for local cancer treatment. FTS-loaded bioresorbable core/shell fiber structures were developed and studied in order to investigate the FTS release mechanism. These structures were composed of a polyglyconate core and a porous poly(d,l-lactic-glycolic acid) shell loaded with FTS, prepared using freeze drying of inverted emulsions. The effects of the emulsion's composition (formulation) and process kinetics on the FTS release from the coatings were studied with reference to the shell morphology and degradation profile. The FTS release profiles exhibited a burst eff... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532326 Sat, 27 Jun 2009 15:57:01 +0100 2532326 http://www.medworm.com/index.php?rid=2532324&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%3D19491027%26dopt%3DAbstract In this study, investigation of the functionality of the outer polymer coating to predict lag time and drug release was statistically analyzed using the response surface methodology (RSM). RSM was employed for designing of the experiment, generation of mathematical models and optimization study. The chosen independent variables, i.e. percentage weight ratios of ethyl cellulose to hydroxypropyl methyl cellulose in the coating formulation and coating level (% weight gain) were optimized with a 3(2) full factorial design. Lag time prior to drug release and cumulative percentage drug release in 7h were selected as responses. Results revealed that both, the coating composition and coating level, are significant factors affecting drug release profile. A second-order polynomial equation fitted to... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532324 Sat, 27 Jun 2009 15:56:58 +0100 2532324 http://www.medworm.com/index.php?rid=2532322&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%3D19491028%26dopt%3DAbstract This study aimed to assess the capability of pluronic surfactants to stabilise topical pressurised hydrofluoroalkane (HFA) emulsions and attempted to define the formulation characteristics that had an impact upon foam properties. In situ phase diagrams and conductivity measurements were used to characterise the HFA emulsions. Cryo-scanning electron microscopy images, collapse time (C(t)) and wetting time (W(t)) were used to assess the foams post dosing, i.e. after removal of the HFA. The results indicated that foam stability was a direct function of HFA emulsion type; HFA-in-water (HIW) emulsions generated stable foams, they had 30-100microm bubble diameter with c.a. 40 bubbles in a 0.45mmx0.40mm area; water-in-HFA (WIH) emulsions created quick-breaking foams they contained 20-200microm si... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532322 Sat, 27 Jun 2009 15:56:54 +0100 2532322 http://www.medworm.com/index.php?rid=2532320&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%3D19491029%26dopt%3DAbstract Authors: Gram LK, Rist GM, Lennernäs H, Steffansen B Carriers may mediate the permeation across enterocytes for drug substances being organic anions. Carrier mediated permeation for the organic anions estrone-3-sulfate (ES) and glipizide across Caco-2 cells were investigated kinetically, and interactions on involved carriers evaluated. Initial uptakes (P(UP)) at apical and basolateral membranes, apparent permeabilities (P(APP)) and corresponding intracellular end-point accumulations (P(EPA)) of radioactive labeled compounds were studied. Possible effects of other anionic compounds were investigated. Apical P(UP) and absorptive P(APP) for ES were inhibited and its absorptive P(EPA) prevented in presence of the investigated organic anions and apical P(UP) was saturable with K(m) 23m... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532320 Sat, 27 Jun 2009 15:56:48 +0100 2532320 http://www.medworm.com/index.php?rid=2532318&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%3D19491030%26dopt%3DAbstract Authors: Wang Y, Chang HI, Li X, Alpar O, Coombes AG Microporous polycaprolactone (PCL) matrices containing lysozyme, collagenase and catalase respectively with molecular weight covering a wide range from 14.3 to 240kDa were produced by a novel method involving rapid cooling of particle suspensions in dry ice. The enzyme loading efficiency (lysozyme (50%), collagenase (75%) and catalase (90%)) depended on the enzyme molecular weight and the non-solvent used to extract acetone from the hardened matrices. Sustained enzyme release occurred from the PCL matrices over 11 days with retained activity dependent on the particular enzyme used (collagenase 100% activity at 11 days, lysozyme 75-80% at 11 days, catalase 10-20% at 5 days). The present findings confirm the potential of microporous PC... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532318 Sat, 27 Jun 2009 15:56:44 +0100 2532318 http://www.medworm.com/index.php?rid=2532316&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%3D19491031%26dopt%3DAbstract Authors: Mulik R, Mahadik K, Paradkar A Curcumininoids, obtained from the rhizomes of Curcuma longa L., Zingiberaceae (turmeric), are the most widely used phytoconstituent in food industry and recently for its therapeutic activity. It has very wide spectrum of therapeutic use like in inflammation, psoriasis, various tumors, wound healing and also in neurodegenerative diseases like Alzheimer's disease. But its highly lipophilic nature and very poor bioavailability hampers its therapeutic usefulness. Poly(butyl) cyanoacrylate (PBCA) nanoparticles coated with poloxamer 188 containing curcuminoids were prepared by anionic polymerization using solvent evaporation method. The particle size and zeta potential of prepared liposomes was 178nm and -28.33 respectively with 77.99% encapsulation ef... European Journal of Pharmaceutical Sciences journals http://www.medworm.com/rss/comments.php?id=2532316 Sat, 27 Jun 2009 15:56:40 +0100 2532316