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 Pharmaceutics and Biopharmaceutics' source. Wed, 08 Feb 2012 14:04:15 +0100 http://www.medworm.com/index.php?rid=5643829&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22285525%26dopt%3DAbstract Authors: Dalmoro A, Barba AA, Lamberti G, d'Amore M Abstract In this review, new approaches to the microencapsulation processes, widely used in the manufacturing of pharmaceutical products, are discussed focusing the attention on the emerging ultrasonic atomization technique. Fundamentals and novel aspects are presented, and advantages of ultrasonic atomization in terms of intensification and low energy requests are emphasized. PMID: 22285525 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5643829 Wed, 25 Jan 2012 05:00:00 +0100 5643829 http://www.medworm.com/index.php?rid=5643830&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22285524%26dopt%3DAbstract Authors: Lademann J, Patzelt A, Schanzer S, Richter H, Thiede G, Havlickova B, Günther C, Friedrich M, Sterry W, Fluhr JW, Seifert S Abstract Bacteria and fungi are located in the stratum corneum and the hair follicles. Therefore, the development and assessment of efficient drugs requires standard in vivo investigation methods permitting a differentiation between intercellular and follicular penetration and storage of topically applied anti-microbial substances. In the present study, the penetration and storage of Isoconazole nitrate in the stratum corneum and hair follicles was investigated by differential stripping after a 14-day topical application period and during a follow-up period of a further 21days. One week after the application had terminated, Isoconazole nitrate could ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5643830 Sat, 21 Jan 2012 05:00:00 +0100 5643830 http://www.medworm.com/index.php?rid=5626111&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22266263%26dopt%3DAbstract Authors: De Zordi N, Moneghini M, Kikic I, Grassi M, Del Rio Castillo AE, Solinas D, Bolger MB Abstract The 'classical' loop diuretic drug Furosemide has been used as a model compound to investigate the possibility of enhancing the dissolution rate of poorly water-soluble drugs using supercritical anti-solvent techniques (SASs). In the present study we report upon the in vitro bioavailability improvement of Furosemide through particle size reduction as well as formation of solid dispersions (SDs) using the hydrophilic polymer Crospovidone. Supercritical carbon dioxide was used as the processing medium for these experiments. In order to successfully design a CO(2) antisolvent process, preliminary studies of Furosemide microparticles generation were conducted using Peng Robinson's Eq... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5626111 Tue, 17 Jan 2012 05:00:00 +0100 5626111 http://www.medworm.com/index.php?rid=5626108&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22269938%26dopt%3DAbstract Authors: Juhnke M, Märtin D, John E Abstract Wet media milling is an established technique for the commercialized top-down production of nanoparticulate drug suspensions. These drug nanosuspensions can be transferred into the related drug products, like capsules, tablets and injectables. The generation of wear during stirred media milling of a drug compound was investigated for grinding media made from yttrium stabilized zirconia. Drug compound and drug nanosuspension were characterized initially by their mechanical and rheological properties. The generation of wear from grinding media has been investigated simultaneously with the reduction of drug particle size by evaluating several grinding media supplier and diameter as well as process parameters stirrer tip speed and specific ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5626108 Tue, 17 Jan 2012 05:00:00 +0100 5626108 http://www.medworm.com/index.php?rid=5626107&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22269939%26dopt%3DAbstract Authors: Saerens L, Dierickx L, Quinten T, Adriaensens P, Carleer R, Vervaet C, Remon JP, Beer TD Abstract The aim was to evaluate near-infrared spectroscopy for the in-line determination of the drug concentration, the polymer-drug solid-state behaviour and molecular interactions during hot-melt extrusion. Kollidon® SR was extruded with varying metoprolol tartrate (MPT) concentrations (20%, 30% and 40%) and monitored using NIR spectroscopy. A PLS model allowed drug concentration determination. The correlation between predicted and real MPT concentrations was good (R(2)=0.97). The predictive performance of the model was evaluated by the root mean square error of prediction, which was 1.54%. Kollidon® SR with 40% MPT was extruded at 105°C and 135°C to evaluate NIR spectroscopy fo... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5626107 Tue, 17 Jan 2012 05:00:00 +0100 5626107 http://www.medworm.com/index.php?rid=5626110&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22269936%26dopt%3DAbstract We report here the intercalation of 5-fluorouracil (5-FU), an anticancer drug in interlayer gallery of Na(+) clay (Montmorillonite, MMT), with the assistance of biopolymer (chitosan, CS). The X-ray diffraction patterns, thermal and spectroscopic analyses indicated the drug intercalation into the clay interlayer space in support of CS and stabilized in the longitudinal monolayer by electrostatic interaction. In vitro drug release showed controlled release pattern. The genotoxic effect of drug was in vitro evaluated in human lymphocyte cell culture by comet assay, and results indicated significant reduction in DNA damage when drug was intercalated with clay and formulated in composites. The results of in vitro cell viability assay in cancer cells pointed at decreased toxicity of drug when en... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5626110 Mon, 16 Jan 2012 05:00:00 +0100 5626110 http://www.medworm.com/index.php?rid=5626109&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22269937%26dopt%3DAbstract In conclusion, moisture plasticization was a highly effective tool to enable the successful compression of pellets coated with the brittle enteric polymer Eudragit® L. PMID: 22269937 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5626109 Mon, 16 Jan 2012 05:00:00 +0100 5626109 http://www.medworm.com/index.php?rid=5626112&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22245573%26dopt%3DAbstract Authors: Sharma K, Somavarapu S, Colombani A, Govind N, Taylor KM Abstract Crosslinked chitosan nanoparticles, prepared using ionic gelation, have been successfully formulated into pressurized metered dose inhalers (pMDIs) with potential for deep lung delivery of therapeutic agents. Nanoparticles were prepared from crosslinked chitosan alone and incorporating PEG 600, PEG 1000 and PEG 5000 for dispersion in aerosol propellant, hydrofuoroalkane (HFA) 227. Spherical, smooth-surfaced, cationic particles of mean size less than 230nm were produced. Nanoparticles were positively charged and non-aggregated at the pH of the airways. Crosslinked chitosan-PEG 1000 nanoparticles demonstrated greatest dispersibility and physical stability in HFA-227, whereas other formulations readily either c... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5626112 Mon, 09 Jan 2012 05:00:00 +0100 5626112 http://www.medworm.com/index.php?rid=5626114&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22245156%26dopt%3DAbstract This article provides a new innovative tool for pharmaceutical preformulation to predict whether a disintegrant excipient or mixture of powder containing API+excipients is suitable to obtain a bucodispersible tablet by direct compression or not. This innovative tool is the new model SeDeM-ODT that provides the Index of Good Compressibility and Bucodispersibility (IGCB index), which is based on the previous SeDeM expert system that indicates the aptitude of a powder to be compressed. The IGCB index is composed of six main factors (from 15 pharmaceutical raw parameters), which indicate whether a mixture of powder has the aptitude to be compressed by direct compression and at the same time indicates whether these tablets are suitable to be used as a bucodispersible tablet (disintegration time... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5626114 Thu, 05 Jan 2012 05:00:00 +0100 5626114 http://www.medworm.com/index.php?rid=5626113&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22245221%26dopt%3DAbstract Authors: Müller J, Brock D, Knop K, Axel Zeitler J, Kleinebudde P Abstract Raman spectroscopy was implemented successfully as a non-invasive and rapid process analytical technology (PAT) tool for in-line quantitative monitoring of functional coating. Coating experiments were performed at which diprophylline tablets were coated with a sustained release formulation based on Kollicoat® SR 30 D. Using PLS a multivariate model was constructed by correlating Raman spectral data with the mean dissolution time as determined by dissolution testing and the coating thickness as measured by terahertz pulsed imaging. By performing in-line measurements it was possible to monitor the progress of the coating process and to detect the end point of the process, where the acquired coating amount wa... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5626113 Thu, 05 Jan 2012 05:00:00 +0100 5626113 http://www.medworm.com/index.php?rid=5580065&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22233547%26dopt%3DAbstract Authors: Salazar J, Ghanem A, Müller RH, Möschwitzer JP Abstract Nanosizing is a non-specific approach to improve the oral bioavailability of poorly soluble drugs. The decreased particle size of these compounds results in an increase in surface area. The outcome is an increased rate of dissolution, which can lead to a better oral absorption. Standard approaches are bottom-up and top-down techniques. Combinative technologies are relatively new approaches, and they can be described as a combination of a bottom-up process followed by a top-down step. The work presented in this paper can be described as a combination of a non-aqueous freeze drying step (bottom-up), followed by wet ball milling or high pressure homogenization (top-down) to produce fine drug nanocrystals. The crystal h... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5580065 Mon, 02 Jan 2012 05:00:00 +0100 5580065 http://www.medworm.com/index.php?rid=5580064&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22233548%26dopt%3DAbstract Authors: Sun DD, Ju TC, Lee PI Abstract The feasibility of forming solid molecular dispersions of poorly water-soluble drugs in crosslinked poly(2-hydroethyl methacrylate) (PHEMA) hydrogel has recently been reported by our group. The purpose of the present study is to investigate the extent of enhancement of kinetic solubility of amorphous solid dispersions (ASDs) of indomethacin (IND) in crosslinked PHEMA hydrogels as compared with those based on conventional water-soluble polymer carriers. Our results show that under non-sink conditions, the initial solubility enhancement is higher for ASDs based on polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose acetate succinate (HMPCAS), but the ability to maintain this solubility enhancement at longer times is better for ASDs base... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5580064 Mon, 02 Jan 2012 05:00:00 +0100 5580064 http://www.medworm.com/index.php?rid=5580066&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22230798%26dopt%3DAbstract Authors: Mortier ST, De Beer T, Gernaey KV, Vercruysse J, Fonteyne M, Remon JP, Vervaet C, Nopens I Abstract The trend to move towards continuous production processes in pharmaceutical applications enhances the necessity to develop mechanistic models to understand and control these processes. This work focuses on the drying behaviour of a single wet granule before tabletting, using a six-segmented fluidised bed drying system, which is part of a fully continuous from-powder-to-tablet manufacturing line. The drying model is based on a model described by Mezhericher et al. [1] and consists of two submodels. In the first drying phase (submodel 1), the surface water evaporates, while in the second drying phase (submodel 2), the water inside the granule evaporates. The second submodel co... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5580066 Sat, 31 Dec 2011 05:00:00 +0100 5580066 http://www.medworm.com/index.php?rid=5580070&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22226681%26dopt%3DAbstract Authors: Yaméogo JB, Gèze A, Choisnard L, Putaux JL, Gansané A, Sirima SB, Semdé R, Wouessidjewe D Abstract We recently reported a one-step transesterification of cyclodextrins (CDs) by vinyl-acyl fatty esters catalyzed by thermolysin. By using the solvent displacement method and depending on the experimental conditions, the CD derivatives grafted with decanoic alkyl chains (CD-C(10)) yielded either nanosphere or nanoreservoir-type systems with a size ranging from 70 to 220nm. Both types of nanostructures were able to associate artemisinin (ART), a well-known antimalarial lipophilic drug. The formulation parameters were optimized to reach stable and high ART dosage corresponding to drug levels of 0.3 and 1.6mgmL(-1) in the colloidal suspension, for the spherical and reservoir-t... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5580070 Fri, 30 Dec 2011 05:00:00 +0100 5580070 http://www.medworm.com/index.php?rid=5580069&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22227367%26dopt%3DAbstract Authors: Devadasu VR, Wadsworth RM, Ravi Kumar MN Abstract The present study is an attempt to leverage therapeutic benefits of curcumin in pulmonary hypertension by encapsulating it in biodegradable poly(lactide-co-glycolic) acid nanoparticles. Pulmonary hypertension is induced in experimental animals by subjecting them to chronic hypoxic conditions. The ability of curcumin encapsulated nanoparticles to manage pulmonary hypertension is measured by right ventricular hypertrophy, haematocrit, vascular remodelling and target tissue levels of curcumin. Further, single oral dose tissue distribution of the nanoparticulate curcumin was also assessed under normoxic and hypoxic conditions. Orally administered nanoparticulate curcumin failed to offer any protection against hypoxia induced pu... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5580069 Fri, 30 Dec 2011 05:00:00 +0100 5580069 http://www.medworm.com/index.php?rid=5580068&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22227368%26dopt%3DAbstract Authors: Bansal SS, Kausar H, Vadhanam MV, Ravoori S, Gupta RC Abstract Curcumin possesses potent anti-inflammatory and anti-proliferative activities but with poor biopharmaceutical attributes. To overcome these limitations, curcumin implants were developed and tissue (plasma, brain and liver) curcumin concentrations were measured in female ACI rats for 3months. Biological efficacy of tissue levels achieved was analyzed by modulation of hepatic cytochromes. Curcumin implants exhibited diffusion-mediated biphasic release pattern with ∼2-fold higher in vivo release as compared to in vitro. Plasma curcumin concentration from implants was ∼3.3ng/ml on day 1, which dropped to ∼0.2ng/ml after 3months, whereas only 0.2-0.3ng/ml concentration was observed from 4-12days with diet and ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5580068 Fri, 30 Dec 2011 05:00:00 +0100 5580068 http://www.medworm.com/index.php?rid=5580067&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22230797%26dopt%3DAbstract Authors: Perioli L, D'Alba G, Pagano C Abstract Furosemide (FURO) is a drug labeled in class IV of the Biopharmaceutics Classification System (BCS) as it is both poor soluble and poor permeable. The aim of this work was to improve FURO biopharmaceutical properties by its formulation in a new solid oral dosage form. It consists in the realization of the composite MgAl-HTlc-FURO, obtained by FURO intercalation into the inorganic matrix hydrotalcite (MgAl-HTlc), and its successive formulation in tablets intended to be swallowed whole and to disintegrate rapidly in the stomach. These formulations were prepared by direct compression of a simple powder mixture constituted by MgAl-HTlc-FURO, a super disintegrant (Explotab®, Polyplasdone®XL, Polyplasdone®XL-10, Polyplasdone®INF 10 or L... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5580067 Fri, 30 Dec 2011 05:00:00 +0100 5580067 http://www.medworm.com/index.php?rid=5567226&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22209978%26dopt%3DAbstract In this study, a reproducible spray-coating process for stents coated with Poly(ethylene carbonate), PEC, and Paclitaxel was investigated. PEC is a biocompatible, thermoelastic polymer of high molecular weight. The surface degradation of PEC is triggered by superoxide anions produced by polymorphonuclear leukocytes and macrophages during inflammatory processes. Stents with different drug loading were reproducibly produced by a spray-coating apparatus. Confocal laser scanning micrographs of fluorescent dye loaded stents were made to investigate the film homogeneity. The abluminal stent site was loaded more than the luminal site, which is superior for DES. The deposition of the layers was confirmed by TOF-SIMS investigations. Referring to the stent surface, the drug loading is 0.32μg (±0.0... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5567226 Wed, 21 Dec 2011 05:00:00 +0100 5567226 http://www.medworm.com/index.php?rid=5567225&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22210473%26dopt%3DAbstract Authors: Marinich JA, Ferrero C, Jiménez-Castellanos MR Abstract A previous paper [1] deals with the physicochemical and technological characterization of novel graft copolymers of ethyl methacrylate (EMA) on waxy maize starch (MS) and hydroxypropylstarch (MHS). The results obtained suggested the potential application of these copolymers as excipients for compressed non-disintegrating matrix tablets. Therefore, the purpose of the present study was to investigate the mechanism governing drug release from matrix systems prepared with the new copolymers and anhydrous theophylline or diltiazem HCl as model drugs with different solubility. The influence of the carbohydrate nature, drying procedure and initial pore network on drug release kinetics was also evaluated. Drug release experi... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5567225 Wed, 21 Dec 2011 05:00:00 +0100 5567225 http://www.medworm.com/index.php?rid=5552414&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22198416%26dopt%3DAbstract Authors: Nafee N, Schneider M, Friebel K, Dong M, Schaefer UF, Muerdter TE, Lehr CM Abstract Antisense oligonucleotide, 2'-O-Methyl-RNA (OMR), is known as potent telomerase inhibitor for the treatment of lung cancer but limited by poor intracellular uptake. Chitosan-coated polymeric nanoparticles were compared to chitosan solution as non-viral vectors for OMR. The study investigated the role of chitosan properties and concentration in improving the efficiency of the nanocarriers in terms of loading, viability, cellular uptake, and telomerase inhibition in human lung cancer cell lines. Certain concentration of chitosan on nanoparticle surface is necessary to significantly increase the cellular uptake. However, excessive chitosan negatively affected the transfection efficiency. Self-... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5552414 Sat, 17 Dec 2011 05:00:00 +0100 5552414 http://www.medworm.com/index.php?rid=5552415&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22198291%26dopt%3DAbstract Authors: Le VN, Robins E, Flament MP Abstract Due to their small size, the respirable drug particles tend to form agglomerates which prevent flowing and aerosolisation. A carrier is used to be mixed with drug in one hand to facilitate the powder flow during manufacturing, in other hand to help the fluidisation upon patient inhalation. Depending on drug concentration, drug agglomerates can be formed in the mixture. The aim of this work was to study the agglomeration behaviour of fluticasone propionate (FP) within interactive mixtures for inhalation. The agglomerate phenomenon of fluticasone propionate after mixing with different fractions of lactose without fine particles of lactose (smaller than 32μm) was demonstrated by the optical microscopy observation. A technique measuring th... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5552415 Wed, 14 Dec 2011 05:00:00 +0100 5552415 http://www.medworm.com/index.php?rid=5538017&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22182528%26dopt%3DAbstract Authors: Nogueiras-Nieto L, Sobarzo-Sánchez E, Gómez-Amoza JL, Otero-Espinar FJ Abstract The competitive interactions between the poly-[propylene oxide] (POO)-poly-[ethylene oxide] (PEO) block copolymer poloxamer 407 (Pluronic F127) and two drugs, triamcinolone acetonide and ciclopirox olamine, by the formation of inclusion complexes with two cyclodextrin hydrophilic derivatives, hydroxypropyl-β-cyclodextrin (HPβCD; molar substitution (MS) 0.65) and partially methylated-β-cyclodextrin (MβCD; MS 0.57), were studied by means of one-dimensional (1)H NMR, 2D ROESY experiments, solubility studies and drug release studies. 1D and 2D NMR and solubility studies indicate that both triamcinolone acetonide and ciclopirox olamine form stable inclusion complexes with the cyclodextrin deri... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538017 Tue, 13 Dec 2011 05:00:00 +0100 5538017 http://www.medworm.com/index.php?rid=5538016&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22193360%26dopt%3DAbstract In this study, uniform mesoporous carbon spheres (UMCS) with 3-D pore system and fibrous ordered mesoporous carbon (FOMC) with 2-dimensional hexagonal mesoporous structure were studied as drug carriers for oral drug delivery system. Lovastatin (LOV), which has low water solubility, was chosen as a model drug. Drug release rate and degree of drug loading of UMCS and FOMC were compared. The effects of different pore channel structures and pore sizes on LOV uptake and release were systematically investigated. Cytotoxicity of UMCS and FOMC on human colon carcinoma (Caco-2) cells were also studied. The results indicate that UMCS has a higher degree of drug loading (up to 36.26% drug weight/total weight) compared with FOMC. The dissolution rate of LOV from UMCS was found to be markedly increased... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538016 Tue, 13 Dec 2011 05:00:00 +0100 5538016 http://www.medworm.com/index.php?rid=5538018&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22178562%26dopt%3DAbstract Authors: Shah M, Ullah N, Choi MH, Kim MO, Yoon SC Abstract Cisplatin is a chemotherapeutic agent used against a variety of tumors. We determined the efficacy and bioavailability of cisplatin in the form of cisplatin-loaded self-assembled amphiphilic copolymer nanoparticles (NPs). Non-crystallizing bacterial copolyester was employed as hydrophobic segment to increase drug loading efficiency. Novel amorphous amphiphilic block copolymer P(3HV-co-4HB)-b-mPEG was synthesized from bacterial copolyester poly(3-hydroxyvalerate-co-4-hydroxybutyrate) coupled via transesterification reaction using bis(2-ethylhexanoate) tin catalyst to monomethoxypoly(ethylene glycol). The product was characterized, and core-shell particles with nanometer size range were prepared by emulsification-solvent eva... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538018 Fri, 09 Dec 2011 05:00:00 +0100 5538018 http://www.medworm.com/index.php?rid=5538020&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155763%26dopt%3DAbstract Authors: Huyge K, Van Reeth K, De Beer T, Landman WJ, van Eck JH, Remon JP, Vervaet C Abstract Dry powders containing a live-attenuated Newcastle disease vaccine (LZ58 strain) and intended for mass vaccination of poultry were prepared by spray drying using mannitol in combination with trehalose or inositol, polyvinylpyrrolidone (PVP) and/or bovine serum albumin (BSA) as stabilizers. These powders were evaluated for vaccine stabilizing capacity during production and storage (at 6°C and 25°C), moisture content, hygroscopicity and dry powder dispersibility. A mixture design, varying the ratio of mannitol, inositol and BSA, was used to select the stabilizer combination which resulted in the desired powder properties (i.e. good vaccine stability during production and storage, low mois... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538020 Wed, 07 Dec 2011 05:00:00 +0100 5538020 http://www.medworm.com/index.php?rid=5538019&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155764%26dopt%3DAbstract Authors: Borde AS, Karlsson EM, Andersson K, Björhall K, Lennernäs H, Abrahamsson B Abstract The aim of this study was to determine the stability of three ester prodrugs, chloramphenicol succinate, enalapril and candesartan cilexetil, in human proximal small intestinal fluid (HIF), dog proximal small intestinal fluids (DIF) and simulated intestinal fluid (FaSSIF), with the addition of pancreatin. The total protein content in the proximal jejunal fluids was determined in HIF and DIF, respectively. Candesartan cilexetil was significantly degraded in HIF (initial t(1/2(0-5min))=5.4±0.5min) and in DIF (initial t(1/2(0-5min))=5.7±0.1min), while chloramphenicol succinate and enalapril were stable in both media. The degradation of candesartan cilexetil was shown to be mediated by enzy... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538019 Sun, 04 Dec 2011 05:00:00 +0100 5538019 http://www.medworm.com/index.php?rid=5538021&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22155591%26dopt%3DAbstract Authors: Rodriguez-Aller M, Kaufmann B, Guillarme D, Stella C, Furrer P, Rudaz S, El Zaoui I, Valamanesh F, Di Tommaso C, Behar-Cohen F, Veuthey JL, Gurny R Abstract Cyclosporine A (CsA) has been demonstrated to be effective for the treatment of a variety of ophthalmological conditions, including ocular surface disorders such as the dry eye disease (DED). Since CsA is characterised by its low water solubility, the development of a topical ophthalmic formulation represents an interesting pharmaceutical question. In the present study, two different strategies to address this challenge were studied and compared: (i) a water-soluble CsA prodrug formulated within an aqueous solution and (ii) a CsA oil-in-water emulsion (Restasis®, Allergan Inc., Irvine, CA). First, the prodrug formulat... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538021 Sat, 03 Dec 2011 05:00:00 +0100 5538021 http://www.medworm.com/index.php?rid=5538023&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22142591%26dopt%3DAbstract Authors: Cagno MD, Stein PC, Styskala J, Hlaváč J, Skalko-Basnet N, Bauer-Brandl A Abstract The pharmaceutical use of some 3-hydroxyquinolinone derivatives with high cytotoxic and cytostatic activities (under in vitro conditions) as well as potential immunosuppressive properties is seriously limited by their low solubility in water accompanied by instability in oxidative environment, like physiological fluids. In an attempt to improve the bioavailability and the stability of four of these derivatives, we propose here two different approaches: complexation with β-cyclodextrin derivatives and incorporation of these substances inside antioxidant micelles. The comparison of the two different methods is the focus of this work, as well as the investigation of some physicochemical prop... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538023 Mon, 28 Nov 2011 05:00:00 +0100 5538023 http://www.medworm.com/index.php?rid=5538022&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22142592%26dopt%3DAbstract Authors: Isacchi B, Bergonzi MC, Grazioso M, Righeschi C, Pietretti A, Severini C, Bilia AR Abstract The therapeutic efficacies of novel liposomal delivery systems based on artemisinin or artemisinin-based combination therapy with curcumin have been investigated and reported in this study. The developed liposomal formulations had proper characteristics as drug carriers for parental administration in terms of particle size, polydispersity, encapsulation efficacy and ζ-potential. Their physical and chemical stabilities were also evaluated. Furthermore, the in vivo antimalarial activity of artemisinin-based liposomal formulations was tested in Plasmodium berghei NK-65 infected mice, a suitable model for studying malaria because the infection presents structural, physiological and lif... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538022 Mon, 28 Nov 2011 05:00:00 +0100 5538022 http://www.medworm.com/index.php?rid=5538025&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22137999%26dopt%3DAbstract In this study, the development of a continuous manufacturing process is described, which can produce grams to kilograms of PCMC. The process chain comprises three steps: mixing/precipitation, solvent reduction (concentration) and final drying. The process is published in two parts. This part describes the mixing and precipitation performed using continuous impingement jet mixers. Mixing efficiency was improved by dividing the anti-solvent flow into two or four jets, which were combined again inside the mixer to achieve an embracing of the aqueous solution (sandwich effect). The jets provided high energy dissipation rates. The anti-solvent jets (95% of the total volume) efficiently mixed the protein-carrier containing aqueous solution (5% of the total volume), which was demonstrated with co... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538025 Sat, 26 Nov 2011 05:00:00 +0100 5538025 http://www.medworm.com/index.php?rid=5538024&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22138000%26dopt%3DAbstract Authors: Casolaro M, Casolaro I, Lamponi S Abstract A series of vinyl hydrogels containing α-aminoacid (l-histidine, l-valine) residues was synthesized and their swelling properties evaluated at different pHs and temperatures. Unlike the zwitterionic compound containing only the l-histidine, a dual-stimuli responsiveness was improved in the carboxyl acid hydrogels carrying the l-valine residues (HVa). Besides the COOH functionality, the presence of either isopropyl and amido groups in the monomer structure renders the hydrogel also temperature-responsive, in a similar manner as the well-known poly(N-isopropylacrylamide) (pNIPAAm). The three HVa hydrogels (cross-linked with 1, 2, and 5mol% of N,N'-ethylene-bisacrylamide, EBA) show a phase separation at the same critical pH4, althou... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538024 Sat, 26 Nov 2011 05:00:00 +0100 5538024 http://www.medworm.com/index.php?rid=5538026&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22137964%26dopt%3DAbstract Authors: Silva SM, Hu L, Sousa JJ, Pais AA, Michniak-Kohn BB Abstract The present work reports the evaluation of three nonionic ether-monohydroxyl surfactants (C(12)E(1), C(12)E(5,) and C(12)E(8)) as skin permeation enhancers in the transdermal drug delivery of two drugs: ondansetron hydrochloride and diltiazem hydrochloride, formulated as hydrogels. The enhancers are used alone, or in combination with iontophoresis (0.3mA - 8h). After 1h of pre-treatment with 0.16M enhancer solutions in propylene glycol (PG), passive and iontophoretic 24h in vitro studies across dermatomed porcine skin were performed using vertical Franz diffusion cells. Data obtained showed that the nonionic surfactant C(12)E(5) was the most effective permeation enhancer, both for the passive process as well as f... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538026 Fri, 25 Nov 2011 05:00:00 +0100 5538026 http://www.medworm.com/index.php?rid=5538027&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22123494%26dopt%3DAbstract Authors: Klang V, Schwarz JC, Lenobel B, Nadj M, Auböck J, Wolzt M, Valenta C Abstract Porcine ear skin is frequently used as a substitute for human skin in dermatological research and is especially useful for tape stripping experiments where the penetration of active substances into the uppermost skin layers is investigated. However, certain differences between the surface properties of these skin types exist, and reports on the comparability of tape stripping data obtained in vitro using porcine ear skin and data obtained in vivo on human forearm skin are scarce. Thus, we performed comparative tape stripping experiments in which the skin penetration of curcumin and fluorescein sodium from conventional microemulsions and hydrogels was investigated. In this context, the skin penet... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538027 Tue, 22 Nov 2011 05:00:00 +0100 5538027 http://www.medworm.com/index.php?rid=5538031&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22119733%26dopt%3DAbstract Authors: Canali MM, Pedrotti LP, Balsinde J, Ibarra C, Correa SG Abstract The intestinal epithelium regulates the transit of molecules from and into the organism. Several agents act as absorption enhancers inducing changes in both transcellular and paracellular routes. Chitosan is a non-toxic biocompatible polysaccharide widely used as dietary supplement and mucosal delivery. Chitosan triggers both the activation of intestinal epithelial cells and the release of regulatory factors relevant for its immunomodulatory activity. Yet, the interaction of chitosan with intestinal epithelial cells is poorly characterized. We studied the uptake of this polysaccharide, and we evaluated its effects in both the net water and ion movements across human and rat colon samples and the epithelial pe... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538031 Sun, 20 Nov 2011 05:00:00 +0100 5538031 http://www.medworm.com/index.php?rid=5538030&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22119734%26dopt%3DAbstract Authors: Wieber A, Selzer T, Kreuter J Abstract In the present study, positively charged 1,2-dioleoyloxy-3-trimethylammoniumpropane (DOTAP) liposomes as a delivery system for a hydrophilic decapeptide were developed. The main objective was the preparation of a stable, highly loaded, lyophilised formulation to yield the basis for an acceptable shelf life. The influences of addition of cholesterol, pH value, amounts of lipid and peptide, type and amount of sugar-based cryoprotective agent (trehalose and sucrose), and time point for cryoprotector addition as well as the freeze-drying process parameters were investigated. The collapse temperatures of the liposome dispersions in the presence of the disaccharides trehalose and sucrose were determined using a freeze-drying microscope (Lyo... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538030 Sun, 20 Nov 2011 05:00:00 +0100 5538030 http://www.medworm.com/index.php?rid=5538028&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22120686%26dopt%3DAbstract This study utilises the methods of cassette dosing and the perfused ovine eye model - to reduce animal usage and therefore animal time - to show that for a series of beta adrenoreceptor antagonists, lipophilicity is a key physicochemical property that governs drug distribution within the eye. Following intravitreal injection, lipophilic beta adrenoreceptor antagonists penetrate to the posterior eye, where they bind to the choroid and reside in the retina at greater concentrations than more hydrophilic beta adrenoreceptor antagonists, which preferentially penetrate to the anterior eye. PMID: 22120686 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538028 Sun, 20 Nov 2011 05:00:00 +0100 5538028 http://www.medworm.com/index.php?rid=5538034&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22119664%26dopt%3DAbstract In conclusion, the addition of poloxamer 188 to pellets containing PVP-based solid dispersions could achieve complete dissolution, accelerated absorption rate and superior oral bioavailability. The fluid-bed technique becomes an alternative approach to obtain solid dispersion-coated pellets. PMID: 22119664 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538034 Fri, 18 Nov 2011 05:00:00 +0100 5538034 http://www.medworm.com/index.php?rid=5538033&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22119665%26dopt%3DAbstract This study therefore provides a novel approach of siRNA delivery to liver hepatocytes, which can also be applied to treat HCV in chronic liver diseases. PMID: 22119665 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538033 Fri, 18 Nov 2011 05:00:00 +0100 5538033 http://www.medworm.com/index.php?rid=5538032&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22119666%26dopt%3DAbstract Authors: Kang JH, Oh DH, Oh YK, Yong CS, Choi HG Abstract In order to investigate the effects of solid carriers on the crystalline properties, dissolution and bioavailability of flurbiprofen in a solid self-nanoemulsifying drug delivery system (solid SNEDDS), different solid SNEDDS formulations were prepared by spray-drying the solutions containing liquid SNEDDS and various carriers. The liquid SNEDDS, composed of Labrafil M 1944 CS/Labrasol/Trasncutol HP (12.5/80/7.5%) with 2%w/v flurbiprofen, gave a z-average diameter of about 100nm. Silicon dioxide, a hydrophobic solid carrier, produced an excellent conventional solid SNEDDS with a nanoemulsion droplet size of less than 100nm, similar to the liquid SNEDDS and smaller than the other solid SNEDDS formulations. The drug was in an a... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538032 Fri, 18 Nov 2011 05:00:00 +0100 5538032 http://www.medworm.com/index.php?rid=5538029&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22120685%26dopt%3DAbstract CONCLUSION: In the present study, absorption of bevacizumab into nasal mucosa was demonstrated, providing new fundamentals that are mandatory for further clinical trials in HHT patients. PMID: 22120685 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5538029 Fri, 18 Nov 2011 05:00:00 +0100 5538029 http://www.medworm.com/index.php?rid=5446106&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22108491%26dopt%3DAbstract The objective of this work is to use a computer simulation in order to test the two approaches. Three pharmacokinetic models, representing different release mechanisms, were considered, and Monte Carlo simulations with intra- and inter-individual variabilities were performed. Five different bioequivalence protocols were used and a new pharmacokinetic metric -C(τ), the concentration at the end of the intended dosing interval obtained in the single-dose study - is proposed in order to avoid the need for steady-state studies while keeping the ability to detect differences between formulations. Results have shown that the European requirements are more capable to discriminate between two potentially different formulations but at the cost of the multiple-dose study and with an increased number... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5446106 Tue, 15 Nov 2011 05:00:00 +0100 5446106 http://www.medworm.com/index.php?rid=5446105&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22108492%26dopt%3DAbstract In this study, we formulated cationic solid lipid nanoparticles (cSLN) for co-delivery of paclitaxel (PTX) and siRNA. 1,2-Dioleoyl-sn-glycero-3-ethylphosphocholine-based cSLN were prepared by emulsification solidification methods. PTX-loaded cSLN (PcSLN) were characterized by zeta potential and gel retardation of complexes with small interfering RNA (siRNA). The sizes of PcSLN did not significantly differ from those of empty cSLN without PTX (EcSLN). The use of cSLN increased the cellular uptake of fluorescent dsRNA in human epithelial carcinoma KB cells, with PcSLN complexed to fluorescence-labeled dsRNA promoting the greatest uptake. For co-delivery of therapeutic siRNA, human MCL1-specific siRNA (siMCL1) was complexed with PcSLN; luciferase-specific siRNA (siGL2) complexed to EcSLN or P... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5446105 Sun, 13 Nov 2011 05:00:00 +0100 5446105 http://www.medworm.com/index.php?rid=5446104&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22108493%26dopt%3DAbstract Authors: Maniruzzaman M, Boateng JS, Bonnefille M, Aranyos A, Mitchell JC, Douroumis D Abstract The purpose of this study was the in vitro and in vivo evaluation of the masking efficiency of hot melt extruded paracetamol (PMOL) formulations. Extruded granules containing high PMOL loadings in Eudragit EPO® (EPO) or Kollidon® VA64 (VA64) were prepared by hot-melt extrusion (HME). The taste masking effect of the processed formulation was evaluated in vivo by a panel of six healthy human volunteers. In addition, in vitro evaluation was carried out by an Astree e-tongue equipped with seven sensors. Taste sensing technology demonstrated taste improvement for both polymers by correlating the data obtained for the placebo polymers and the pure APIs alone. The best masking effect was obse... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5446104 Sun, 13 Nov 2011 05:00:00 +0100 5446104 http://www.medworm.com/index.php?rid=5446107&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22101181%26dopt%3DAbstract This study has focused on the synthesis and in vitro characterization of a targeting delivery system of 5-fluorouracil (5-FU) to human head and neck squamous cell carcinoma (HNSCC) in order to improve anti-cancer efficacy and reduce dose-limiting toxicity of 5-FU. An N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer, with Hsp47/CBP2 binding peptide sequence (namely WHYPWFQNWAMA) as a targeting ligand, was synthesized by a novel and simplified synthetic route. Under the controlled synthetic conditions, 1,3-dimethylol-5-FU, derived from 5-FU, was attached to the HPMA copolymer backbone via the lysosomally degradable GFLG linker, while the WHYPWFQNWAMA was conjugated via a non-degradable Gly-Gly (GG) linker. A control polymer without targeting moiety was also synthesized (P-FU). The in vitr... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5446107 Sat, 12 Nov 2011 05:00:00 +0100 5446107 http://www.medworm.com/index.php?rid=5427067&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085653%26dopt%3DAbstract In conclusion, a high and rapid cellular uptake was shown for siRNA-loaded nanoparticles. Cell internalization is based on an energy-dependent and predominantly clathrin-mediated process. Particle localization in endosomes and lysosomes was demonstrated. Evidence for the efficient delivery of bioactive siRNA and specific GFP knockdown provides a solid basis for the application of DEAPA-PVA-g-PLGA-based particles for gene silencing in vivo. PMID: 22085653 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5427067 Thu, 10 Nov 2011 05:00:00 +0100 5427067 http://www.medworm.com/index.php?rid=5427066&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22085654%26dopt%3DAbstract Authors: Shapira A, Davidson I, Avni N, Assaraf YG, Livney YD Abstract We studied a potential drug delivery system comprising the hydrophobic anticancer drug paclitaxel entrapped within β-casein (β-CN) nanoparticles and its cytotoxicity to human gastric carcinoma cells. Paclitaxel was entrapped by stirring its dimethyl sulfoxide (DMSO) solution into PBS containing β-CN. Cryo-TEM analysis revealed drug nanocrystals, the growth of which was blocked by β-CN. Entrapment efficiency was nearly 100%, and the nanovehicles formed were colloidally stable. Following encapsulation and simulated digestion with pepsin (2 hours at pH=2, 37°C), paclitaxel retained its cytotoxic activity to human N-87 gastric cancer cells; the IC(50) value (32.5±6.2nM) was similar to that of non-encapsulated ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5427066 Wed, 09 Nov 2011 05:00:00 +0100 5427066 http://www.medworm.com/index.php?rid=5427068&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22079174%26dopt%3DAbstract Authors: Schloegl W, Klein A, Fürst R, Leicht U, Volkmer E, Schieker M, Jus S, Guebitz GM, Stachel I, Meyer M, Wiggenhorn M, Friess W Abstract In the present study, we developed an enzyme-linked immunosorbent assay (ELISA) for microbial transglutaminase (mTG) from Streptomyces mobaraensis to overcome the lack of a quantification method for mTG. We further performed a detailed follow-on-analysis of insoluble porcine collagen type I enzymatically modified with mTG primarily focusing on residuals of mTG. Repeated washing (4×) reduced mTG-levels in the washing fluids but did not quantitatively remove mTG from the material (p<0.000001). Substantial amounts of up to 40% of the enzyme utilized in the crosslinking mixture remained associated with the modified collagen. Binding was non... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5427068 Fri, 04 Nov 2011 04:00:00 +0100 5427068 http://www.medworm.com/index.php?rid=5427070&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22068049%26dopt%3DAbstract In conclusion, the proposed Ni-NCs can bind His-tagged proteins and have the potential to be used as antigen delivery system capable of generating strong antigen-specific antibodies at doses much lower than with aluminum-based adjuvant and causing no significant elevation of systemic pro-inflammatory IL-12/p40 and CCL5/RANTES cytokines. PMID: 22068049 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5427070 Mon, 31 Oct 2011 04:00:00 +0100 5427070 http://www.medworm.com/index.php?rid=5427069&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22068050%26dopt%3DAbstract In this study, the low-cost production of recombinant human erythropoietin cysteine analogs (Cys-rhEPOs) from Pichia pastoris and the potential to increase their serum residency and in vivo activity through cysteine-specific PEGylation were investigated. Three-dimensional structures of several Cys-rhEPOs were generated using homology modeling, and three stable Cys-rhEPOs were selected on the basis of model stability in molecular dynamics simulation and surface accessibility of the inserted cysteine. cDNAs encoding Cys-rhEPOs were constructed by site-directed mutagenesis and expressed as secreted proteins in flask cultures of P. pastoris. The selection of highly expressing clones and the optimization of certain culture parameters resulted in protein expression levels of 100-170mg/l. Purifie... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5427069 Mon, 31 Oct 2011 04:00:00 +0100 5427069 http://www.medworm.com/index.php?rid=5427073&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22061261%26dopt%3DAbstract Authors: Sun F, Li J, Yu Q, Chan E Abstract 3-Deazaneplanocin A (DZNep) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein. The purpose of this study was to improve the pharmacokinetic characteristics of DZNep in vivo through developing a unilamellar pegylated liposomal formulation encapsulating DZNep (L-DZNep). A remote-loading method in the presence of phenylboronic acid (R-w-PBA) was developed to stably encapsulating DZNep inside liposomes (encapsulation efficiency=50.7% at molar ratio of 1:10 of drug to lipids) through forming a transient PBA-DZNep complex. The pharmacokinetics of L-DZNep was investigated in Sprague-Dawley rats. In comparison with free drug, encapsulation of the DZNep in pegylated lipos... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5427073 Fri, 28 Oct 2011 04:00:00 +0100 5427073 http://www.medworm.com/index.php?rid=5427072&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22061262%26dopt%3DAbstract Authors: Esposito E, Mariani P, Ravani L, Contado C, Volta M, Bido S, Drechsler M, Mazzoni S, Menegatti E, Morari M, Cortesi R Abstract The physico-chemical properties and in vivo efficacies of two nanoparticulate systems delivering the antiparkinsonian drug bromocriptine (BC) were compared in the present study. Monoolein aqueous dispersions (MADs) and Nanostructured Lipid Carrier (NLC) were produced and characterized. Cryogenic transmission electron microscopy (cryo-TEM) and X-ray diffraction revealed the morphology of MAD and NLC. Dimensional distribution was determined by Photon Correlation Spectroscopy (PCS) and Sedimentation Field Flow Fractionation (SdFFF). In particular, BC was shown to be encapsulated with high entrapment efficiency both in MAD and in NLC, according to SdFF... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5427072 Fri, 28 Oct 2011 04:00:00 +0100 5427072 http://www.medworm.com/index.php?rid=5427071&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22061263%26dopt%3DAbstract In this study, to improve the brain drug delivery and reduce the immunogenicity of traditional lectin modified delivery system, Odorranalectin (OL, 1700Da), a novel non-immunogenic small peptide, was selected to establish an OL-modified cubosomes (Cubs) system. The streptavidin (SA)-conjugated Cubs were prepared by incorporating maleimide-PEG-oleate and taking advantage of its thiol group binding reactivity to conjugate with 2-iminothiolane thiolated SA; mono-biotinylated OL was then coupled with the SA-modified Cubs. The OL-decorated Cubs (OL-Cubs) devised via a non-covalent SA-biotin "bridge" made it easy to conjugate OL and determine the number of ligands on the surface of the Cubs using sensitive chemiluminescent detection. Retention of the bio-recognitive activity of OL after covalent... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5427071 Fri, 28 Oct 2011 04:00:00 +0100 5427071 http://www.medworm.com/index.php?rid=5383113&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041602%26dopt%3DAbstract Authors: Janga KY, Jukanti R, Velpula A, Sunkavalli S, Bandari S, Kandadi P, Veerareddy PR Abstract The present systematic study focused to investigate the combined advantage of proliposomes and surface charge for improved oral delivery of zaleplon. The zaleplon loaded proliposomes were prepared using hydrogenated soyphosphatidylcholine (HSPC) and cholesterol (CHOL) in varying ratios, and the optimized formulation was tailored with dicetyl phosphate and stearylamine to obtain negative and positive charged vesicles, respectively. The formulations were characterized for micromeritics, size, zeta potential, and entrapment efficiency. Further, in vitro release and dissolution study carried out provide an insight on the stability and enhanced dissolution of zaleplon from proliposome for... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5383113 Tue, 25 Oct 2011 04:00:00 +0100 5383113 http://www.medworm.com/index.php?rid=5383114&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041601%26dopt%3DAbstract In this study, we intended to encapsulate topotecan within liposome adopting transmembrane NH(4)EDTA gradient in order to increase the antitumor activity and decrease the toxicity against normal immune organs. Regarding the encapsulation efficiency of topotecan liposomes, both the pH value of the buffer and the cholesterol content showed significant effects on encapsulation and drug retention. Liposome encapsulation dramatically increased the antitumor activity of topotecan compared to free drug (p<0.05), while similar efficacy was obtained from liposomes prepared by a NH(4)EDTA gradient or a (NH(4))(2)SO(4) gradient (tumor inhibition ratios were 85.6% and 84.1%, respectively). However, a significant decrease in toxicity against the immune organs was found in liposomes prepared by a NH(... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5383114 Mon, 24 Oct 2011 04:00:00 +0100 5383114 http://www.medworm.com/index.php?rid=5363415&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22036988%26dopt%3DAbstract Authors: Murata M, Nakano K, Tahara K, Tozuka Y, Takeuchi H Abstract The aim of this study was to investigate the feasibility of surface-modified liposomes for pulmonary delivery of a peptide. Chitosan oligosaccharide (oligoCS) and polyvinyl alcohol with a hydrophobic anchor (PVA-R) were used as surface modifiers. The effect of liposomal surface modification on the behavior of the liposomes on pulmonary administration and potential toxicity were evaluated in vitro and in vivo. In an association study with A549 cells, PVA-R modification reduced interaction with A549 cells, whereas oligoCS modification electrostatically enhanced cellular interaction. The therapeutic efficacy of elcatonin (eCT) after pulmonary administration to rats was significantly enhanced and prolonged for 48h aft... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363415 Thu, 20 Oct 2011 04:00:00 +0100 5363415 http://www.medworm.com/index.php?rid=5363414&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22036989%26dopt%3DAbstract Authors: Vilela FM, Fonseca YM, Jabor JR, Vicentini FT, Fonseca MJ Abstract Organic sunscreens may decrease their protective capability and also behave as photo-oxidants upon ultraviolet radiation (UVR) exposure. The present study investigated the effect of a cream gel formulation containing the UV filters benzophenone-3, octyl methoxycinnamate, and octyl salicylate on skin superoxide dismutase (SOD) after a single dose of UVR (2.87J/cm(2)). The retention of these UV filters was first evaluated in vivo using hairless mice to guarantee the presence of the filters in the skin layers at the moment of irradiation. The in vivo effect of the UV filters on skin SOD was then assayed spectrophotometrically via the reduction of cytochrome c. The cream gel formulation promoted the penetration... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363414 Thu, 20 Oct 2011 04:00:00 +0100 5363414 http://www.medworm.com/index.php?rid=5363413&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22036990%26dopt%3DAbstract Authors: Tay T, Morton DA, Gengenbach TR, Stewart PJ Abstract The purpose of this research was to investigate the influence of dry coating micronized cohesive powders of a poorly water-soluble drug, indomethacin with force control agents, on its dissolution performance. A dry mechanical fusion method (mechanofusion) was used to coat indomethacin powders with magnesium stearate (0.25%,1%,5%) and sodium stearate (5%). After mechanofusion, significantly increased bulk and tapped densities and decreased intrinsic cohesion were observed for all samples. X-ray photoelectron spectroscopy analysis confirmed that a thicker magnesium stearate surface coating was achieved with increasing concentrations of the material. Dissolution was studied using the USP paddle method in buffer pH 5.0; seve... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363413 Thu, 20 Oct 2011 04:00:00 +0100 5363413 http://www.medworm.com/index.php?rid=5363417&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22024407%26dopt%3DAbstract In this study, non-ionic surfactants, pluronic F68 (PF68) and Tween 80 (TW80), were used to address this limitation. The human CC cell line, HuCC-T1, was cotreated with ALA and different concentrations of surfactants for 4h. The effect of surfactants was evaluated by monitoring the uptake of ALA, the fluorescence intensity of PpIX, and the cell survival rate after suitable light irradiation. Cotreatment with the surfactant resulted in an increased intracellular ALA level, PpIX formation, and phototoxicity. PMID: 22024407 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363417 Tue, 18 Oct 2011 04:00:00 +0100 5363417 http://www.medworm.com/index.php?rid=5363416&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22024408%26dopt%3DAbstract Authors: Mohanan D, Gander B, Kündig TM, Johansen P Abstract During the last two decades, synthetic polymers such as poly(lactide-co-glycolide) (PLGA) have been investigated for the development of nano- or microparticles as adjuvants or antigen vehicles. To enable transfer of this technology to human settings, the issue of sterilisation will soon be of central importance. Since most polymers are heat-sensitive, sterilisation of polymeric microspheres for parenteral administration is assured either by costly and laborious aseptical preparation or the more preferred γ-irradiation. Many studies have investigated the effect of γ-irradiation on various physiochemical properties of the microspheres, but investigations on immunological effects are rare. We prepared poly(lactide-co-glyc... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363416 Tue, 18 Oct 2011 04:00:00 +0100 5363416 http://www.medworm.com/index.php?rid=5363419&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22019529%26dopt%3DAbstract Authors: Karmwar P, Graeser K, Gordon KC, Strachan CJ, Rades T Abstract The aim of this study was to investigate whether amorphous indomethacin samples prepared using different preparative techniques and processing parameters exhibit different structural and thermodynamic characteristics and whether these differences can be correlated to their dissolution behaviour. Samples were prepared either by cooling the drug melt at different cooling rates or by cryo-milling the drug for different milling times. The resulting amorphous materials were characterised using X-ray diffraction, Raman spectroscopy and polarising light microscopy. All samples were entirely X-ray amorphous, except for the sample cryo-milled for 15min, which exhibited residual crystallinity. The shape of the halos in t... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363419 Fri, 14 Oct 2011 04:00:00 +0100 5363419 http://www.medworm.com/index.php?rid=5363418&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22019530%26dopt%3DAbstract In this study, we evaluated the usefulness of biorelevant in vitro data and of canine data in forecasting early exposure after the administration of two phases of a BCS Class II compound, i.e., doxazosin base (DB) and its mesylate salt (DM). DB, DM, and doxazosin hydrochloride (DH) were prepared and characterized. In vitro data were collected in various media, including human aspirates. Solubilities of DB and DM in human gastric fluid were forecasted by data in fasted state simulating gastric fluid containing physiological components (FaSSGF-V2) but not by data in HCl(pH 1.8). Unlike data in FaSSGF-V2, dissolution of DB and DM tablets in HCl(pH 1.6) is rapid. Dissolution of DB tablet in FaSSGF-V2 is incomplete and conversion to DH seems to occur. Differences between DB and DM in dissolutio... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363418 Fri, 14 Oct 2011 04:00:00 +0100 5363418 http://www.medworm.com/index.php?rid=5363423&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22005155%26dopt%3DAbstract Authors: Simões SM, Veiga F, Torres-Labandeira JJ, Ribeiro AC, Sandez-Macho MI, Concheiro A, Alvarez-Lorenzo C Abstract The ability of Pluronic® F127 to form supramolecular gels in the presence of αCD has been explored as a way to design syringeable gel formulations able to sustain drug release while using the lowest proportion of both components. The effects of αCD concentration range (0-9.7%w/v) in copolymer (6.5%, 13% and 20%) gel features were evaluated at 4, 20 and 37°C. An effective complexation of Pluronic and αCD was evidenced as a change in the surface pressure of the π-A isotherm of Pluronic on a subphase of CD solution and the apparition of new peaks in the X-ray spectra. Once the Pluronic and αCD solutions were mixed, the systems became progressively turbid solu... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363423 Sat, 08 Oct 2011 04:00:00 +0100 5363423 http://www.medworm.com/index.php?rid=5363422&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22008146%26dopt%3DAbstract Authors: Güres S, Siepmann F, Siepmann J, Kleinebudde P Abstract The aim of this study was to use a mechanistically realistic mathematical model based on Fick's second law to quantitatively predict the release profiles from solid lipid extrudates consisting of a ternary matrix. Diprophylline was studied as a freely water-soluble model drug, glycerol tristearate as a matrix former and polyethylene glycol or crospovidone as a pore former (blend ratio: 50:45:5%w/w/w). The choice of these ratios is based on former studies. Strains with a diameter of 0.6, 1, 1.5, 2.7 and 3.5mm were prepared using a twin-screw extruder at 65°C and cut into cylinders of varying lengths. Drug release in demineralised water was measured using the USP 32 basket apparatus. Based on SEM pictures of extrudate... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363422 Sat, 08 Oct 2011 04:00:00 +0100 5363422 http://www.medworm.com/index.php?rid=5363421&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22008147%26dopt%3DAbstract Authors: Stella B, Arpicco S, Rocco F, Burgalassi S, Nicosia N, Tampucci S, Chetoni P, Cattel L Abstract The aim of this study was to increase bioavailability of the antiviral drug acyclovir (ACV) when administered by the ocular route. For this purpose, a new lipophilic derivative of acyclovir was synthesized, both possessing greater lipophilicity and providing the formation of a homogeneous water dispersion with higher amount of ACV than the aqueous solution of the parent drug. This was done by chemically linking acyclovir to the isoprenoid chain of squalene, obtaining 4'-trisnorsqualenoylacyclovir (SQACV), in which squalene is covalently coupled to the 4'-hydroxy group of acyclovir. This new prodrug was then formulated as nonpolymeric nanoassemblies through nanoprecipitation; the... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363421 Sat, 08 Oct 2011 04:00:00 +0100 5363421 http://www.medworm.com/index.php?rid=5363420&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22008148%26dopt%3DAbstract Authors: Onoue S, Sato H, Ogawa K, Kojo Y, Aoki Y, Kawabata Y, Wada K, Mizumoto T, Yamada S Abstract The main purpose of the present study was to develop a novel respirable powder (RP) formulation of cyclosporine A (CsA) using a spray-dried O/W-emulsion (DE) system. DE formulation of CsA (DE/CsA) was prepared by spray-drying a mixture of erythritol and liquid O/W emulsion containing CsA, polyvinylpyrrolidone, and glyceryl monooleate as emulsifying agent. The DE/CsA powders were mixed with lactose carriers to obtain an RP formulation of DE/CsA (DE/CsA-RP), and its physicochemical, pharmacological, and pharmacokinetic properties were evaluated. Spray-dried DE/CsA exhibited significant improvement in dissolution behavior with ca. 4500-fold increase of dissolution rate, and then, nanoe... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363420 Sat, 08 Oct 2011 04:00:00 +0100 5363420 http://www.medworm.com/index.php?rid=5363424&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22001519%26dopt%3DAbstract Authors: Mueannoom W, Srisongphan A, Taylor KM, Hauschild S, Gaisford S Abstract The use of thermal ink-jet spray freeze-drying (TIJ-SFD) to engineer inhalable, excipient-free salbutamol sulphate (SS) particles was assessed. A modified Hewlett-Packard printer was used to atomise aqueous SS solutions into liquid nitrogen. The frozen droplets were freeze-dried. It was found that TIJ-SFD could process SS solutions up to 15%w/v; the porous particles produced had a physical diameter of ca. 35μm. Next generation impactor (NGI) analysis indicated that the particles had a smaller aerodynamic size (MMAD ranging from 6 to 8.7μm). Particles prepared from the lowest concentration SS solution were too fragile to withstand aerosolisation, but the 5%w/v solution yielded particles having the bes... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363424 Fri, 07 Oct 2011 04:00:00 +0100 5363424 http://www.medworm.com/index.php?rid=5363425&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22000996%26dopt%3DAbstract Authors: Benzeval I, Bowyer A, Hubble J Abstract The interactions of a number of commercially available dextran preparations with the lectin Concanavalin A (ConA) have been investigated. Dextrans over the molecular mass range 6×10(3)-2×10(6)gmol(-1) were initially characterised in terms of their branching and hence terminal ligand density, using NMR. This showed a range of branching ratios between 3% and 5%, but no clear correlation with molecular mass. The bio-specific interaction of these materials with ConA was investigated using microcalorimetry. The data obtained were interpreted using a number of possible binding models reflecting the known structure of both dextran and the lectin. The results of this analysis suggest that the interaction is most appropriately described in ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5363425 Thu, 06 Oct 2011 04:00:00 +0100 5363425 http://www.medworm.com/index.php?rid=5283952&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21439376%26dopt%3DAbstract We describe a novel method to fabricate pH-responsive microparticles suitable for oral delivery using an aqueous-based spray-drying approach. The approach involves the neutralization and generation of water-soluble salt forms of enteric polymers. The methacrylic acid polymers (Eudragit L and Eudragit S) were added separately to aqueous solutions of ammonium hydrogen carbonate; the solutions were then spray-dried. FTIR analysis of the harvested microparticle products identified the presence of ammonium methacrylate with the appearance of a peak at 1550cm(-1) corresponding to the stretching of the N-H bond. Incubating the microparticles for three hours at 70°C and 130°C for the Eudragit S and L products, respectively, was sufficient to eradicate the ammonium residues. The microparticles, l... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283952 Sat, 01 Oct 2011 04:00:00 +0100 5283952 http://www.medworm.com/index.php?rid=5283951&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21443951%26dopt%3DAbstract Authors: Li Y, McClements DJ Abstract The effect of low-molecular weight surfactants on the digestibility of lipids in protein-stabilized corn oil-in-water emulsions was studied using an in vitro digestion model. The impact of non-ionic (Tween 20, Tween 80, Brij35), anionic (SDS), and cationic (DTAB) surfactants on the rate and extent of lipid digestion was studied. All surfactants were found to inhibit lipid digestion at sufficiently high concentrations, with half-maximal inhibitory concentrations (IC50) of 1.2% for Tween 20, 0.7% for Tween 80, 2.8% for Brij35, 1.1% for SDS, and 1.4% for DTAB. The effectiveness of the surfactants at inhibiting lipid digestion was therefore not strongly correlated to the electrical characteristics of the surfactant head group, since the IC50 increa... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283951 Sat, 01 Oct 2011 04:00:00 +0100 5283951 http://www.medworm.com/index.php?rid=5283950&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21458565%26dopt%3DAbstract Authors: Wells LA, Sheardown H Abstract Covalent modification of alginate with polyethylene glycol-conjugated anthracene molecules has the potential to both stabilize the alginate and act as a photosensitive crosslinker. Release studies with Coomassie Blue show lengthy release times from the alginate photogels that extend past 70days with, for example, 17% versus 27% release at 1750h (73days) for photogels with and without 365-nm UV light treatment for 30min at 10mW/cm(2) in the initial release period. Photocrosslinking of the photogels after loading effectively "locks" in drug compounds to control their release. Effective crosslinking densities and controls of polyethylene glycol-crosslinked alginate and physically crosslinked calcium alginate gels suggest strong interactions betw... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283950 Sat, 01 Oct 2011 04:00:00 +0100 5283950 http://www.medworm.com/index.php?rid=5283949&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21458566%26dopt%3DAbstract Authors: Lin X, Chyi CW, Ruan KF, Feng Y, Heng PW Abstract This work aimed to explore the potential of lactose as novel cushioning agents with suitable physicomechanical properties by micronization and co-spray drying with polymers for protecting coated multi-particulates from rupture when they are compressed into tablets. Several commercially available lactose grades, micronized lactose (ML) produced by jet milling, spray-dried ML (SML), and polymer-co-processed SMLs, were evaluated for their material characteristics and tableting properties. Hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC), and polyvinylpyrrolidone (PVP) at three different levels were evaluated as co-processed polymers for spray drying. Sugar multi-particulates layered with chlorpheniramine malea... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283949 Sat, 01 Oct 2011 04:00:00 +0100 5283949 http://www.medworm.com/index.php?rid=5283948&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21458567%26dopt%3DAbstract Authors: Berbicz F, Nogueira AC, Neto AM, Natali MR, Baesso ML, Matioli G Abstract This work is aimed to evaluate the application of photoacoustic spectroscopy (PAS) in the characterization of inclusion complexes of benzophenone-3 (BZ-3) and hydroxypropyl-β-cyclodextrin (HPCD) and to analyze the ex vivo percutaneous penetration of sunscreens and their reaction with the skin. The formation of inclusion complexes of BZ-3 and HPCD was performed by co-precipitation in stoichiometric ratios of 1:1 and 1:2. Thermal analysis and PAS characterized these inclusion complexes, and they indicated that the stoichiometric ratio of 1:2 was best. Sunscreen formulations were prepared and applied on the ears of rabbits. PAS suggested that the formulation with the complex resulted in lower penetrati... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283948 Sat, 01 Oct 2011 04:00:00 +0100 5283948 http://www.medworm.com/index.php?rid=5283947&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21540110%26dopt%3DAbstract This study demonstrates that PCA can be successfully applied to ToF-SIMS data from different ocular tissues and highlights the potential of coupling multivariate statistics with surface analytical techniques to gain a greater understanding of the biochemical composition of tissues and the distribution of pharmaceutically active small molecules within these tissues. PMID: 21540110 [PubMed - in process] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283947 Sat, 01 Oct 2011 04:00:00 +0100 5283947 http://www.medworm.com/index.php?rid=5283946&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21549839%26dopt%3DAbstract Authors: Fischer SM, Brandl M, Fricker G Abstract Drug permeability of the model drugs ketoprofen and nadolol across Caco-2 cell monolayers was determined in the absence and presence of the non-ionic surfactant Poloxamer 188 (Pluronic® F68, P-188). Stringent controls confirmed that P-188 in concentrations up to 50mg/ml did not adversely affect cell viability or monolayer integrity. Equilibrium experiments confirmed that the drugs were merely passively transported. Caco-2 permeability of both drugs was found to be decreased by the surfactant in a concentration-dependent manner. Ultrafiltration revealed that both drugs were associated with surfactant micelles. The systematic investigation of micellization on passive absorption showed that association of drugs with P-188 micelles app... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283946 Sat, 01 Oct 2011 04:00:00 +0100 5283946 http://www.medworm.com/index.php?rid=5283945&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21550400%26dopt%3DAbstract Authors: Luciani P, Fevre M, Leroux JC Abstract Istaroxime, an investigational new drug that targets defective Ca(2+) cycling without compromising cardiac efficiency, may represent a promising and safe treatment of both acute and chronic heart failure. Even though the compound demonstrated good tolerability in a phase I/II safety study, symptoms related to the gastro-intestinal tract and pain at the injection site were reported as the most frequent side effects. The aim of this study was to encapsulate istaroxime in a drug delivery system (DDS) that could minimize the pain perceived upon administration. The DDS was designed to be quickly destabilized in plasma, in order to minimize alteration of the pharmacokinetic profile of istaroxime. To meet those requirements, a balance betwee... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283945 Sat, 01 Oct 2011 04:00:00 +0100 5283945 http://www.medworm.com/index.php?rid=5283944&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21550401%26dopt%3DAbstract The objectives of this study was to prepare solid self-nanoemulsifying drug delivery system (S-SNEDDS) containing phosphatidylcholine (PC), an endogenous phospholipid with excellent in vivo solubilization capacity, as oil phase for the delivery of bioactive carotenoid lutein, by spray drying the SNEDDS (liquid system) containing PC using colloidal silica (Aerosil® 200 VV Pharma) as the inert solid carrier, and to evaluate the enhanced bioavailability (BA) of lutein from S-SNEDDS. The droplet size analyses revealed droplet size of less than 100nm. The solid state characterization of S-SNEDDS by SEM, DSC, and XRPD revealed the absence of crystalline lutein in the S-SNEDDS. The bioavailability study performed in rabbits resulted in enhanced values of C(max) and AUC for S-SNEDDS. The enhancem... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283944 Sat, 01 Oct 2011 04:00:00 +0100 5283944 http://www.medworm.com/index.php?rid=5283937&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21964315%26dopt%3DAbstract This study also shows that informative structural characterisation is possible for adjuvant bound sub-unit vaccines. PMID: 21964315 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283937 Thu, 22 Sep 2011 04:00:00 +0100 5283937 http://www.medworm.com/index.php?rid=5283936&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21964316%26dopt%3DAbstract Authors: Iqbal J, Shahnaz G, Perera G, Hintzen F, Sarti F, Bernkop-Schnürch A Abstract The aim of the present study was to develop an oral delivery system for the peptide drug leuprolide. Gel formulations based on unmodified chitosan/reduced glutathione (GSH) and chitosan-thioglycolic acid (chitosan-TGA)/GSH were prepared, and their effect on the absorption of leuprolide was evaluated in vitro and in vivo in male Sprague Dawley rats. Transport studies were performed with freshly excised rat intestinal mucosa mounted in Ussing-type chambers. Due to the addition of gel formulations comprising 0.5% (m/v) unmodified chitosan/0.5% (m/v) GSH and 0.5% (m/v) chitosan-TGA/0.5% (m/v) GSH, the transport of leuprolide across excised mucosa was improved up to 2.06-fold and 3.79-fold, respectiv... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283936 Thu, 22 Sep 2011 04:00:00 +0100 5283936 http://www.medworm.com/index.php?rid=5283935&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21964317%26dopt%3DAbstract In conclusion, this work demonstrates the suitability of photocrosslinked poly(ester anhydride)s for use in peptide delivery. PMID: 21964317 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283935 Thu, 22 Sep 2011 04:00:00 +0100 5283935 http://www.medworm.com/index.php?rid=5283938&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21964202%26dopt%3DAbstract Authors: Govedarica B, Sovány T, Pintye-Hódi K, Skarabot M, Baumgartner S, Muševič I, Srčič S Abstract Our goal was to understand and thus be able to predict the swelling behavior of xanthan matrix tablets in media of various pH and ionic strengths using data obtained from single xanthan molecules and films with atomic force microscopy. Imaging was performed in 1-butanol using contact mode AFM in order to characterize single xanthan chains prepared from various solutions. Image analysis was used to calculate the molecular contour, persistence length, and radius of gyration. Nanoindentation measurements of xanthan films were carried out to evaluate their mechanical properties. Increasing the ionic strength of solutions induced reductions in chain parameters such as molecular c... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283938 Wed, 21 Sep 2011 04:00:00 +0100 5283938 http://www.medworm.com/index.php?rid=5283941&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21946473%26dopt%3DAbstract Authors: Aguilar-de-Leyva A, Cifuentes C, Rajabi-Sihabbomi AR, Caraballo I Abstract Percolation theory has been applied to estimate the Hypromellose (HPMC) percolation thresholds and the influence of the polymer viscosity and the initial porosity on these thresholds in carbamazepine multicomponent matrix formulations. Different batches containing two viscosity grades of HPMC as hydrophilic matrix forming polymer, MCC and lactose as fillers, and a lubricant mixture have been manufactured varying the compression pressure in order to obtain matrices with three levels of initial porosity. The results suggested the existence of an excipient percolation threshold between 13 and 15% v/v of HPMC for the different batches prepared. It has been found that the percolation threshold for this p... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283941 Sat, 17 Sep 2011 04:00:00 +0100 5283941 http://www.medworm.com/index.php?rid=5283940&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21946474%26dopt%3DAbstract Authors: Nordström J, Klevan I, Alderborn G Abstract In this paper, a structured protocol for powder compression analysis as a test to assess the mechanical properties of particles in a formulation development programme is presented. First, the sequence of classification steps of the protocol is described, and secondly, the protocol is illustrated using compression data of six powders of two model substances, sodium chloride and mannitol. From powder compression data, a set of compression variables are derived, and by using critical values of these variables, the stages expressed during the compression of the powders are identified and the powders are classified into groups with respect to the expression of particle rearrangement, particle fragmentation and particle plastic deform... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283940 Sat, 17 Sep 2011 04:00:00 +0100 5283940 http://www.medworm.com/index.php?rid=5283942&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21946301%26dopt%3DAbstract Authors: Morais T, Elisa Soares M, Duarte JA, Soares L, Maia S, Gomes P, Pereira E, Fraga S, Carmo H, Bastos MD Abstract Successful application of gold nanoparticles (AuNPs) in biomedicine requires extensive safety assessment for which biokinetic studies are crucial. We evaluated the biodistribution of AuNPs (∼20nm) with different surface coatings: citrate, 11-MUA and 3 pentapeptides, CALNN, CALND and CALNS, after i.v. administration to rats (0.6-1mg Au/kg). Biodistribution was evaluated based on Au tissue content measured by GFAAS. Citrate-AuNPs were rapidly removed from circulation with 60% of the injected dose depositing in the liver. Thirty minutes post-injection, the lungs presented about 6% of the injected dose with levels decreasing to 0.7% at 24h. Gold levels in the splee... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283942 Fri, 16 Sep 2011 04:00:00 +0100 5283942 http://www.medworm.com/index.php?rid=5283943&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21945270%26dopt%3DAbstract In this study we investigated the stability and release properties of biodegradable polylactic acid (PLA) particles upon topical application on human skin explants. PLA particles loaded with the hydrophilic fluorochrome 4-Di-2-Asp (DiAsp-PLA) were compared to PLA particles loaded with the lipophilic fluorochrome Bodipy 630/650 (BP-PLA). Changes of the particle morphology after their incubation on skin surface were investigated by means of electron microscopy while fluorescence microscopy and flow cytometry were used to evaluate particle penetration in hair follicles and fluorochrome release. We found that BP-PLA particles released rapidly the loaded fluorochrome and lost the particulate morphology within a few hours after application on skin surface. On the contrary, DiAsp-PLA particles ma... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283943 Wed, 14 Sep 2011 04:00:00 +0100 5283943 http://www.medworm.com/index.php?rid=5283939&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21945271%26dopt%3DAbstract Authors: Baumann D, Bachert C, Högger P Abstract For locally acting drugs, an extended residence time in the nasal cavity is desirable and related to a prolonged effect. We sought to develop a model for comparative determination of intranasal pharmacokinetics. We embedded human respiratory tissue into a solid matrix and coated the surface with artificial nasal fluid. Nasal spray suspensions of fluticasone propionate (FP) and budesonide (Bud) as well as a solution of azelastine hydrochloride (AZ) were applied onto the surface and removed after 30min to simulate mucociliary clearance. As exemplary anti-inflammatory measure, we evaluated the inhibition of IL-8 release from epithelial cells. FP and Bud were initially bound to the same extent to the tissue gel while AZ displayed a more... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5283939 Wed, 14 Sep 2011 04:00:00 +0100 5283939 http://www.medworm.com/index.php?rid=5249605&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21939763%26dopt%3DAbstract The objective of this work was to develop and evaluate simple pharmaceutical bases stabilized with natural-origin surfactant of alkyl polyglucoside (APG) type as prospective ready-to-use bases and compare them to widely used pharmacopoeial ones. Additionally, the ability of the formulated bases to sustain isopropyl alcohol was assessed as well as its influence on ketoprofen skin absorption (as a co-solvent and potential penetration enhancer). In order to evaluate the manifold characteristics a topical drug product should possess, a comprehensive characterization was performed using different techniques. Physicochemical characterization demonstrated satisfactory physical stability of APG-stabilized bases upon the addition of alcohol. In vitro release/permeation studies failed to show signif... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5249605 Sat, 10 Sep 2011 04:00:00 +0100 5249605 http://www.medworm.com/index.php?rid=5234789&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21924354%26dopt%3DAbstract Authors: Said SS, El-Halfawy OM, El-Gowelli HM, Aloufy AK, Boraei NA, El-Khordagui LK Abstract Despite innovation in the design and functionalization of polymer nanofiber wound healing materials, information on their interaction with the biochemical wound environment is lacking. In an earlier study, we have reported the interaction of fusidic acid-loaded PLGA ultrafine fibers (UFs) with wound bacteria. Massive bacterial colonization and the formation of a dense biofilm throughout the mat were demonstrated. This was associated with a marked enhancement of initial drug release at concentrations allowing eradication of planktonic bacteria and considerable suppression of biofilm. The present study aimed at extending earlier findings to gain more mechanistic insights into the potential ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5234789 Thu, 08 Sep 2011 04:00:00 +0100 5234789 http://www.medworm.com/index.php?rid=5234787&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21924356%26dopt%3DAbstract The objective of this study was therefore to reduce the rate of evaporation of the oil via microencapsulation. Microcapsules (MCs) were prepared using gelatin simple coacervation method and sodium sulfate (20%) as a coacervating agent. The MCs were hardened with a cross-linking agent, formaldehyde (37%). The effects of three variables, stirring rate, oil loading and the amount of cross-linking agent, on encapsulation efficiency (EE, %) were studied. Response surface methodology was employed to optimize the EE (%), and a polynomial regression model equation was generated. The effect of the amount of cross-linker was insignificant on EE (%). The response surface plot constructed for the polynomial equation provided an optimum area. The MCs under the optimized conditions provided EE of 60%. T... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5234787 Thu, 08 Sep 2011 04:00:00 +0100 5234787 http://www.medworm.com/index.php?rid=5234788&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21924355%26dopt%3DAbstract In conclusion, we have identified approaches to achieve formulation and colloidal stability of OEI-HD/siRNA complexes, a step toward successful application of polyplexes for in vivo siRNA delivery. PMID: 21924355 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5234788 Tue, 06 Sep 2011 04:00:00 +0100 5234788 http://www.medworm.com/index.php?rid=5221360&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21907802%26dopt%3DAbstract Authors: Rehder S, Sakmann A, Rades T, Leopold CS Abstract A glibenclamide polymorph published by Panagopoulou-Kaplani and Malamataris (2000) [1], obtained by sublimation of amorphous glibenclamide, was analysed. A new interpretation of the data is presented and experimentally confirmed by X-ray powder diffraction, Fourier transformation infrared spectroscopy, differential scanning calorimetry, and mass spectrometry. The crystals formed during sublimation of amorphous glibenclamide do not represent a glibenclamide polymorph, but a thermal degradation product, namely 1,3-dicyclohexylurea. The reaction mechanism is suggested to be an elimination of cyclohexylisocyanate from glibenclamide. Cyclohexylisocyanate may decompose to carbon monoxide and cyclohexylamine, which may react in an... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5221360 Fri, 02 Sep 2011 04:00:00 +0100 5221360 http://www.medworm.com/index.php?rid=5180228&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21872135%26dopt%3DAbstract Authors: Gurny R, Leroux JC PMID: 21872135 [PubMed - in process] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5180228 Wed, 31 Aug 2011 23:00:00 +0100 5180228 http://www.medworm.com/index.php?rid=5160226&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21864681%26dopt%3DAbstract Authors: Mennini N, Furlanetto S, Cirri M, Mura P Abstract The aim of the present work was to develop a new multiparticulate system, designed for colon-specific delivery of celecoxib for both systemic (in chronotherapic treatment of arthritis) and local (in prophylaxis of colon carcinogenesis) therapy. The system simultaneously benefits from ternary complexation with hydroxypropyl-β-cyclodextrin and PVP (polyvinylpyrrolidone), to increase drug solubility, and vectorization in chitosan-Ca-alginate microspheres, to exploit the colon-specific carrier properties of these polymers. Statistical experimental design was employed to investigate the combined effect of four formulation variables, i.e., % of alginate, CaCl(2), and chitosan and time of cross-linking on microsphere entrapment e... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5160226 Mon, 15 Aug 2011 23:00:00 +0100 5160226 http://www.medworm.com/index.php?rid=5142618&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21846502%26dopt%3DAbstract Authors: Hentzschel CM, Alnaief M, Smirnova I, Sakmann A, Leopold CS Abstract The potential of hydrophilic aerogel formulations and liquisolid systems to improve the release of poorly soluble drugs was investigated using griseofulvin as model drug. The in vitro release rates of this drug formulated as directly compressed tablets containing crystalline griseofulvin were compared to aerogel tablets with the drug adsorbed onto hydrophilic silica aerogel and to liquisolid compacts containing the drug dissolved or suspended in PEG 300. Furthermore, the commonly used carrier and coating materials in liquisolid systems Avicel® and Aerosil® were replaced by Neusilin®, an amorphous magnesium aluminometasilicate with an extremely high specific surface area of 339m(2)/g to improve the liqu... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5142618 Mon, 08 Aug 2011 23:00:00 +0100 5142618 http://www.medworm.com/index.php?rid=5142619&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21839833%26dopt%3DAbstract Development of a new delivery system consisting in "drug - in cyclodextrin - in nanostructured lipid carriers" for ketoprofen topical delivery. Eur J Pharm Biopharm. 2011 Aug 4; Authors: Cirri M, Bragagni M, Mennini N, Mura P Abstract A new delivery system based on drug cyclodextrin (Cd) complexation and loading into nanostructured lipid carriers (NLC) has been developed to improve ketoprofen therapeutic efficacy. The proposed strategy exploits both the solubilizing and stabilizing properties of Cds and the prolonged release, high tolerability and percutaneous absorption enhancer properties of NLC. Two different polymeric Cds, i.e. β-Cd-epichlorohydrin polymer (EPI-βCd) and carboxymethylathed-β-Cd-epichlorohydrin polymer (EPI-CMβCd) were tested and two different techniq... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5142619 Wed, 03 Aug 2011 23:00:00 +0100 5142619 http://www.medworm.com/index.php?rid=5109033&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21791369%26dopt%3DAbstract This study revealed that the produced keratin film offers a possibility as a human nail plate substitute. However, inclusion of the penetration enhancer must be carefully interpreted. PMID: 21791369 [PubMed - in process] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5109033 Sun, 31 Jul 2011 23:00:00 +0100 5109033 http://www.medworm.com/index.php?rid=5109032&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21801834%26dopt%3DAbstract The objective of this study was the development of retarded release pellets using vegetable calcium stearate (CaSt) as a thermoplastic excipient. The matrix carrier was hot melt extruded and pelletized with a hot-strand cutter in a one step continuous process. Vegetable CaSt was extruded at temperatures between 100 and 130°C, since at these temperatures cutable extrudates with a suitable melt viscosity may be obtained. Pellets with a drug loading of 20% paracetamol released 11.54% of the drug after 8h due to the great densification of the pellets. As expected, the drug release was influenced by the pellet size and the drug loading. To increase the release rate, functional additives were necessary. Therefore, two plasticizers including glyceryl monostearate (GMS) and tributyl citrate (TBC)... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5109032 Tue, 26 Jul 2011 23:00:00 +0100 5109032 http://www.medworm.com/index.php?rid=5109029&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21820510%26dopt%3DAbstract Authors: Tripathi SK, Goyal R, Ansari KM, Ravi Ram K, Shukla Y, Chowdhuri DK, Gupta KC A series of polyethylenimine (PEI) and γ-polyglutamic acid (PGA) nanocomposites (PPGA) was prepared and evaluated in terms of their cell viability and transfection efficiency in vitro and in vivo. On complexion with pDNA, the positively charged PPGA/DNA nanocomposites resulted in a higher level of in vitro reporter gene transfection (2.7-7.9-fold) as compared to native PEI, and selected commercial reagents and >95% cell viability in HEK293, HeLa and HepG2 cell lines. Further, PPGA-5 nanocomposite (the best working system in terms of transfection efficiency among the series) was found to efficiently transfect primary mouse keratinocytes up to 22% above the control level. PPGA-5, when tested for in... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5109029 Tue, 26 Jul 2011 23:00:00 +0100 5109029 http://www.medworm.com/index.php?rid=5109028&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21820511%26dopt%3DAbstract Authors: Asmus LR, Gurny R, Möller M Solid poly(lactides) and poly(lactide-co-glycolides) are widely used polymers for sustained-release parenterals. However, they have some unfavorable properties regarding manufacturing of the formulations and administration to the patient due to their solid aggregate state. In contrast, hexyl-substituted poly(lactic acid) (hexPLA, poly(2-hydroxyoctanoic acid)) is a viscous degradable polyester. To date, a two-step ring-opening polymerization was used for its synthesis. Here, we investigated a novel one-pot one-step melt polycondensation method to prepare hexPLA for biomedical applications by a simple green chemistry process. No catalyst or solely pharmaceutically acceptable catalysts and environmentally friendly purification methods without organic ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5109028 Mon, 25 Jul 2011 23:00:00 +0100 5109028 http://www.medworm.com/index.php?rid=5109031&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21820051%26dopt%3DAbstract Authors: Tozuka Y, Imono M, Uchiyama H, Takeuchi H The effectiveness of α-glucosyl hesperidin (Hsp-G) as a novel grinding aid for the preparation of drug nanoparticles by dry grinding was investigated. Poorly water-soluble drugs and Hsp-G were mixed at a weight ratio of 1/5 and ground for 60min by a vibrational ball mill. It was evident that all poorly water-soluble drugs used in this study formed nanoparticles after the ground mixtures were dispersed into distilled water. The dissolution profile of glibenclamide from the ground mixtures of glibenclamide/Hsp-G showed dramatic improvement from that of untreated drug crystals. Administration of the ground mixture of glibenclamide/Hsp-G to rats resulted in a significantly higher rate of decrease in blood glucose levels than that of untre... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5109031 Sat, 23 Jul 2011 23:00:00 +0100 5109031 http://www.medworm.com/index.php?rid=5109030&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21820052%26dopt%3DAbstract Authors: Lai F, Pini E, Angioni G, Manca ML, Perricci J, Sinico C, Fadda AM In this paper, orally disintegrating tablets (ODT) were prepared using nanocrystal formulations in order to optimise dissolution properties of lipophilic, poorly soluble drug piroxicam (PRX). Different nanocrystal formulations were prepared using a high pressure homogenisation technique and poloxamer 1888 as stabiliser. Characterisation of PRX nanocrystal ODT was carried out by infrared spectroscopy (FTIR), X-ray powder diffractometry (XRPD), differential scanning calorimetry and photon correlation spectroscopy. Dissolution study of PRX ODT was performed in distilled water (pH 5.5) and was compared to that of PRX coarse suspension ODT, PRX/poloxamer 188 physical mixture and bulk PRX samples. The XRPD and FTIR s... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5109030 Sat, 23 Jul 2011 23:00:00 +0100 5109030 http://www.medworm.com/index.php?rid=5067207&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21784150%26dopt%3DAbstract Authors: Bildstein L, Pili B, Marsaud V, Wack S, Meneau F, Lepêtre-Mouelhi S, Desmaële D, Bourgaux C, Couvreur P, Dubernet C We have designed an amphiphilic prodrug of the anticancer agent gemcitabine (dFdC), by covalent coupling to squalene. This bioconjugate, which self-assembled into nanoparticles (NPs) in water, was previously found to display an impressive anticancer activity both in vitro and in vivo. The present study aims to investigate the impact of SQdFdC nanoparticles on cellular membranes. MTT assays showed that, in the nanomolar range, squalenoyl gemcitabine (SQdFdC) was slightly less active than dFdC on a panel of human cancer cell lines, in vitro. However, above 10μmolL(-1) SQdFdC was considerably more cytotoxic than dFdC. Contrarily to its parent drug, SQdFdC also in... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5067207 Mon, 18 Jul 2011 23:00:00 +0100 5067207 http://www.medworm.com/index.php?rid=5067206&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21784151%26dopt%3DAbstract Authors: Lin X, Wang ZJ, Wang S, Shen L, Feng Y, Ruan KF, Xu DS PEGylation was found to be a promising approach to improve the anti-myocardial ischemic activity of Radix Ophiopogonis polysaccharide (ROP) by prolonging its retention in plasma. To fully evaluate the effectiveness and safety of this strategy, the tissue distribution of PEGylated ROP was investigated in this study. A long-circulating and bioactive PEGylated ROP with 1.04mol 20-kDa mPEG per mol ROP ((1.04)P(20k)-R) was prepared by a moderate coupling reaction between the hydroxyl-activated ROP and the amino-terminated mPEG. Its tissue distribution in mice with normal and ischemic myocardium was studied and compared with ROP. The results show that the descending order of tissue distribution of (1.04)P(20k)-R ranked by AUC wa... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5067206 Mon, 18 Jul 2011 23:00:00 +0100 5067206 http://www.medworm.com/index.php?rid=5067208&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21767643%26dopt%3DAbstract Authors: Hu Y, Zhi Z, Wang T, Jiang T, Wang S In the present study, we exploited for the first time the potential of 3-D ordered macroporous (3DOM) silica as matrix for drug nanoparticles, in order to obtain proper control over drug particle size in the sub-micrometer range, enhance the dissolution rate, and reduce gastric damage. 3DOM silica matrix with 3-D spherical pores of 200nm was successfully created and then loaded with IMC nanoparticles at various drug-silica ratios. A rapid release profile for IMC nanoparticle formulations was achieved in comparison with micronized IMC and a commercial capsule, which could be attributed to both increase in the specific surface area and decrease in the crystallinity of IMC, as well as the hydrophilic surface and the interconnected pore network... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5067208 Thu, 14 Jul 2011 23:00:00 +0100 5067208 http://www.medworm.com/index.php?rid=5067209&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21757004%26dopt%3DAbstract Authors: Borde A, Larsson A, Holmgren J, Nygren E Different oral liquid cholera vaccines have proved to be safe and effective, but their formulations present problems for use in low-income countries, since large package volumes have to be transported and cold chain maintenance is required. A solid state formulation would here be more advantageous, and consequently, the possibility to develop a dry cholera vaccine formulation by freeze-drying was investigated. The ability of sucrose, trehalose and mannitol to provide process stabilization during freeze-drying was tested on a formalin-killed whole-cell Vibrio cholerae model vaccine. A matrix of sucrose or trehalose prevented bacterial aggregation, preserved cell morphology and maintained practically completely the protective lipopolysacc... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5067209 Sat, 02 Jul 2011 23:00:00 +0100 5067209 http://www.medworm.com/index.php?rid=5067210&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21745568%26dopt%3DAbstract Authors: Wacker C, Berger CN, Girard P, Meier R Recombinant antibodies specific for human targets are often used as therapeutics and represent a major class of drug products. Their therapeutic efficacy depends on the formation of antibody complexes resulting in the elimination of a target molecule or the modulation of specific signalling pathways. The physiological effects of antibody therapeutics are known to depend on the structural characteristics of the antibody molecule, specifically on the glycosylation which is the result of posttranslational modifications. Hence, production of therapeutic antibodies with a defined and consistent glycoform profile is needed which still remains a considerable challenge to the biopharmaceutical industry. To provide an insight into the industries c... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5067210 Fri, 01 Jul 2011 23:00:00 +0100 5067210 http://www.medworm.com/index.php?rid=5015049&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21736941%26dopt%3DAbstract Authors: Yang Y, Zhao W, He J, Zhao Y, Ding F, Gu X Incorporation of nerve growth factor (NGF) into a nerve conduit can improve peripheral nerve regeneration. Here, genipin, a natural and low toxic agent, was used to crosslink chitosan, a natural polysaccharide, and concurrently to immobilize NGF onto modified chitosan, followed by fabrication of chitosan (CS)-genipin (GP)-NGF nerve conduits. MTT test showed that the cell viability of Schwann cells cultured in the conduit extract was not significantly different from that in plain medium. The neurite outgrowth measurement and immunocytochemistry with anti-growth-associated protein-43 and anti-neurofilament indicated that NGF released from CS-GP-NGF nerve conduits retained the bioactivity of stimulating neuronal differentiation of PC12 c... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5015049 Sun, 26 Jun 2011 23:00:00 +0100 5015049 http://www.medworm.com/index.php?rid=5015050&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21736940%26dopt%3DAbstract This study is designed to test the hypothesis that tenofovir (TNF) or tenofovir disoproxil fumarate (TDF) loaded nanoparticles (NPs) prepared with a blend of poly(lactic-co-glycolic acid) (PLGA) and methacrylic acid copolymer (Eudragit® S-100, or S-100) are noncytotoxic and exhibit significant pH-responsive release of anti-HIV microbicides in the presence of human semen. After NPs preparation by emulsification diffusion, their size, encapsulation efficiency (EE%), drug release profile, morphology, and cytotoxicity are characterized by dynamic light scattering, spectrophotometry, transmission electron microscopy, and cellular viability assay/transepithelial electrical resistance measurement, respectively. Cellular uptake was elucidated by fluorescence spectroscopy and confocal microscopy. ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5015050 Sat, 25 Jun 2011 23:00:00 +0100 5015050 http://www.medworm.com/index.php?rid=5015051&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21726641%26dopt%3DAbstract Authors: Delgado D, Del Pozo-Rodríguez A, Solinís MA, Gascón AR The aim of our study was to evaluate the effect of protamine on the transfection capacity of solid lipid nanoparticles (SLNs) by correlating it to the internalization mechanisms and intracellular trafficking of the vectors. Vectors were prepared with SLN, DNA, and protamine. ARPE-19 and HEK-293 cells were used for the evaluation of the formulations. Protamine induced a 6-fold increase in the transfection of SLNs in retinal cells due to the presence of nuclear localization signals (NLS), its protection capacity, and a shift in the internalization mechanism from caveolae/raft-mediated to clathrin-mediated endocytosis. However, protamine produced an almost complete inhibition of transfection in HEK-293 cells. In spite of t... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5015051 Fri, 24 Jun 2011 23:00:00 +0100 5015051 http://www.medworm.com/index.php?rid=5015052&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21723945%26dopt%3DAbstract In conclusion, the bioadhesive films formed from organic-inorganic hybrid gels possessed very good qualities for application on the skin and may provide a promising formulation for TDDS, especially when the patient acceptability from an aesthetic perspective of the dosage form is a prime consideration. PMID: 21723945 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5015052 Thu, 23 Jun 2011 23:00:00 +0100 5015052 http://www.medworm.com/index.php?rid=5015053&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21723390%26dopt%3DAbstract In this study, linear homopolymers of N-ethyl pyrrolidine methacrylamide (EPA), copolymers of EPA with N,N-dimethylacrylamide (DMA) and oligomers of EPA were synthesized, and the resulting structures were evaluated for their transfection efficiency as non-viral gene vectors. Specifically, polymer species with high and low molecular weights (120-2.6kDa) and different functionalities (tertiary amines as side chains and primary amine as chain end) were prepared as non-crosslinked, linear homopolymers, copolymers and oligomers, respectively. Polymer/DNA complexes (polyplexes) formation was evaluated by agarose gel electrophoresis, showing that all systems complexed with DNA in all P/N ratios with the exception of the EPA homopolymer. Furthermore, light scattering measurements and transmission ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5015053 Wed, 22 Jun 2011 23:00:00 +0100 5015053 http://www.medworm.com/index.php?rid=5015055&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21703347%26dopt%3DAbstract Authors: Mueller C, Capelle MA, Arvinte T, Seyrek E, Borchard G Protein aggregation, which is triggered by various factors, is still one of the most prevalent problems encountered during all stages of protein formulation development. In this publication, we present novel excipients, tryptophan-mPEGs (Trp-mPEGs) of 2 and 5kDa molecular weight and suggest their use in protein formulation. The synthesis and physico-chemical characterization of the excipients are described. Possible cytotoxic and hemolytic activities of the Trp-mPEGs were examined. Turbidity, 90° static light scatter, intrinsic fluorescence, fluorescence after staining the samples with Nile Red and fluorescence microscopy were used to study the inhibitory effect of the Trp-mPEGs on the aggregation of salmon calcitonin (sC... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5015055 Mon, 13 Jun 2011 23:00:00 +0100 5015055 http://www.medworm.com/index.php?rid=5015054&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21703348%26dopt%3DAbstract The objective of this work was to investigate the influence of various micronized, poorly water-soluble, inorganic materials on the dissolution and de-agglomeration behavior of a micronized, poorly water-soluble model drug, indomethacin, from lactose interactive mixtures. Dissolution of indomethacin was studied using the USP paddle method, and the data were modeled with multi-exponential equations using a nonlinear least squares algorithm in order to obtain key parameter estimates. The dispersion of indomethacin mixtures was measured by laser diffraction. The addition of aluminum hydroxide and calcium phosphate to binary mixtures of indomethacin counter-intuitively improved the dissolution rate of indomethacin due to significant increases in both the estimated initial concentration and dis... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=5015054 Mon, 13 Jun 2011 23:00:00 +0100 5015054 http://www.medworm.com/index.php?rid=4969298&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21693188%26dopt%3DAbstract Authors: Sakuma S, Higashino H, Oshitani H, Masaoka Y, Kataoka M, Yamashita S, Hiwatari KI, Tachikawa H, Kimura R, Nakamura K, Kumagai H, Gore JC, Pham W We have designed a novel colonoscopic imaging agent that is composed of submicron-sized fluorescent polystyrene nanospheres with two functional groups - peanut agglutinin (PNA) and poly(N-vinylaceamide) (PNVA) - on their surfaces. PNA is a targeting moiety that binds to β-d-galactosyl-(1-3)-N-acetyl-d-galactosamine (Gal-β(1-3)GalNAc), which is the terminal sugar of the Thomsen-Friedenreich antigen that is specifically expressed on the mucosal side of colorectal cancer cells; it is anchored on the nanosphere surface via a poly(methacrylic) acid (PMAA) linker. PNVA is immobilized to enhance the specificity of PNA by reducing nonspecif... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4969298 Sun, 12 Jun 2011 23:00:00 +0100 4969298 http://www.medworm.com/index.php?rid=4969297&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21693189%26dopt%3DAbstract Authors: Alhusban F, Perrie Y, Mohammed AR The current study aimed to exploit the electrostatic associative interaction between carrageenan and gelatin to optimise a formulation of lyophilised orally disintegrating tablets (ODTs) suitable for multiparticulate delivery. A central composite face centred (CCF) design was applied to study the influence of formulation variables (gelatin, carrageenan and alanine concentrations) on the crucial responses of the formulation (disintegration time, hardness, viscosity and pH). The disintegration time and viscosity were controlled by the associative interaction between gelatin and carrageenan upon hydration which forms a strong complex that increases the viscosity of the stock solution and forms tablet with higher resistant to disintegration in aqu... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4969297 Sun, 12 Jun 2011 23:00:00 +0100 4969297 http://www.medworm.com/index.php?rid=4969299&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21683790%26dopt%3DAbstract In conclusion, the combination of absorption enhancers and electrical assistance is a potential strategy for the enhancement of transbuccal sCT delivery. PMID: 21683790 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4969299 Sat, 11 Jun 2011 23:00:00 +0100 4969299 http://www.medworm.com/index.php?rid=4969300&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21664970%26dopt%3DAbstract Authors: Mortier ST, De Beer T, Gernaey KV, Remon JP, Vervaet C, Nopens I Fluidized bed dryers are frequently used in industrial applications and also in the pharmaceutical industry. The general incentives to develop mechanistic models for pharmaceutical processes are listed, and our vision on how this can particularly be done for fluidized bed drying processes of wet granules is given. This review provides a basis for future mechanistic model development for the drying process of wet granules in pharmaceutical processes. It is intended for a broad audience with a varying level of knowledge on pharmaceutical processes and mathematical modelling. Mathematical models are powerful tools to gain process insight and eventually develop well-controlled processes. The level of detail embedded ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4969300 Wed, 01 Jun 2011 23:00:00 +0100 4969300 http://www.medworm.com/index.php?rid=4969302&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21664462%26dopt%3DAbstract Authors: Sandolo C, Péchiné S, Monnier AL, Hoys S, Janoir C, Coviello T, Alhaique F, Collignon A, Fattal E, Tsapis N We have designed an oral vaccine against Clostridium difficile infection. The virulent factor Cwp84, that is a cystein protease highly immunogenic in patients with C. difficile-associated disease, was entrapped within pectin beads. Beads encapsulating Cwp84 were shown to be stable in the simulated intestinal medium and to release the cystein protease once in the simulated colonic medium. Three groups of hamsters were immunized, the first receiving pectin beads encapsulating Cwp84, the second unloaded beads and the third one free Cwp84. After three immunizations by the intragastric route, all groups received clindamycine. Post-challenge survival with a strain of C. diff... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4969302 Tue, 31 May 2011 23:00:00 +0100 4969302 http://www.medworm.com/index.php?rid=4969301&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21664463%26dopt%3DAbstract Authors: Jensen LB, Petersson K, Nielsen HM Treatment of skin diseases implies application of a drug to skin with an impaired epidermal barrier, which is likely to affect the penetration profile of the drug substance as well as the carrier into the skin. To elucidate this, the effect of skin barrier damage on the penetration profile of a corticosteroid applied in solid lipid nanoparticles (SLN) composed of different lipids, varying in polarity, was studied. The studies were carried out in vitro using impaired and intact porcine ear skin, and the SLN were compared with a conventional ointment. It was shown that a significantly higher amount of corticosteroid remained in the skin, intact as well as barrier impaired, when SLN was used as a vehicle. In general, the penetration profile of t... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4969301 Mon, 30 May 2011 23:00:00 +0100 4969301 http://www.medworm.com/index.php?rid=4922497&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21645616%26dopt%3DAbstract Authors: Cespi M, Bonacucina G, Mencarelli G, Casettari L, Palmieri GF It is common practice to coat oral solid dosage forms with polymeric materials for controlled release purposes or for practical and aesthetic reasons. Good knowledge of thermo-mechanical film properties or their variation as a function of polymer grade, type and amount of additives or preparation method is of prime importance in developing solid dosage forms. This work focused on the dynamic mechanical thermal characteristics of free films of hypromellose 2910 (also known as HPMC), prepared using three grades of this polymer from two different manufacturers, in order to assess whether polymer chain length or origin affects the mechanical or thermo-mechanical properties of the final films. Hypromellose free films wer... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4922497 Sun, 29 May 2011 23:00:00 +0100 4922497 http://www.medworm.com/index.php?rid=4922496&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21658448%26dopt%3DAbstract Authors: Groen D, Poole DS, Gooris GS, Bouwstra JA The lipids in the uppermost layer of the skin, the stratum corneum (SC), play an important role in the barrier function. The main lipid classes in stratum corneum are ceramides, cholesterol, and free fatty acids. In previous publications, a lipid model was presented, referred to as the stratum corneum substitute (SCS), that closely mimics the SC lipid organization and SC barrier function. In the present study, we use the SCS to study the effect of changes in lipid organization on the lipid barrier function using benzoic acid as permeation compound. First, in the SCS, we increased the level of one of the three major lipid classes keeping the ratio between the other lipid classes constant. An increased cholesterol level resulted in an in... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4922496 Sun, 29 May 2011 23:00:00 +0100 4922496 http://www.medworm.com/index.php?rid=4922495&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21658449%26dopt%3DAbstract In conclusion, the nanomatrix formulation described here is a promising system to enhance the oral bioavailability of water-insoluble drugs. PMID: 21658449 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4922495 Sun, 29 May 2011 23:00:00 +0100 4922495 http://www.medworm.com/index.php?rid=4922499&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21640187%26dopt%3DAbstract Authors: Vandamme K, Melkebeek V, Cox E, Adriaensens P, Van Vlierberghe S, Dubruel P, Vervaet C, Remon JP The adjuvant effect of methylvinylether-co-maleic anhydride (Gantrez®AN) nanoparticles was investigated during oral vaccination of mice with F4 adhesins of F4-positive Escherichia coli. To differentiate whether the adjuvant effect originated from a nanoparticle effect or a polymer effect, 20μgF4 was administered as slightly crosslinked F4-containing nanoparticles (g(F4)(0.01)) or as F4 mixed with slightly crosslinked pure nanoparticles (F4+g(0.01)). The F4-specific immune response was reduced using F4-containing nanoparticles due to complete shielding of F4, whereas oral administration of F4+g(0.01) increased the level of F4-specific antibody-secreting cells (ASC) in the spleen. ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4922499 Thu, 26 May 2011 23:00:00 +0100 4922499 http://www.medworm.com/index.php?rid=4922498&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21641994%26dopt%3DAbstract In conclusion, it was demonstrated that both the in situ gelling formulation evaluated and the chitosan solution are viable alternatives to enhance ocular bioavailability in the treatment of fungal keratitis. PMID: 21641994 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4922498 Thu, 26 May 2011 23:00:00 +0100 4922498 http://www.medworm.com/index.php?rid=4922501&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21620969%26dopt%3DAbstract In conclusion, this study demonstrated the efficiency of the calixarene nanoemulsion, which can be regarded as a promising treatment for uranium cutaneous contamination. PMID: 21620969 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4922501 Wed, 18 May 2011 23:00:00 +0100 4922501 http://www.medworm.com/index.php?rid=4922500&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21620970%26dopt%3DAbstract Authors: Plesner B, Fee CJ, Westh P, Nielsen AD The effects of PEGylation on the structural, thermal and functional stability of bovine serum albumin (BSA) were investigated using BSA and 6 linear mono-PEGylated BSA compounds. The secondary and tertiary structure of BSA measured by circular dichroism (CD) was independent of PEGylation. In contrast, the thermal stability of BSA was affected by PEGylation. The apparent unfolding temperature T(max) measured by differential scanning calorimetry (DSC) decreased with PEGylation, whereas the temperature of aggregation, T(agg), measured by dynamic light scattering (DLS) increased with PEGylation. The unfolding temperature and the temperature of aggregation were both independent of the molecular weight of the PEG chain. Possible functional chan... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4922500 Tue, 17 May 2011 23:00:00 +0100 4922500 http://www.medworm.com/index.php?rid=4876798&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21605671%26dopt%3DAbstract Authors: Fontana MC, Rezer JF, Coradini K, Leal DB, Beck RC We developed a dermatological nanomedicine containing clobetasol propionate-loaded nanocapsules and evaluated its efficacy in a model of contact dermatitis after topical administration in rats. Hydrogels containing clobetasol propionate-loaded lipid-core nanocapsules or nanoemulsion (HG-CP-NC and HG-CP-NE, respectively) were prepared to evaluate the influence of the polymeric wall. They presented adequate pH values (5.50-6.50) and drug content (0.5mgg(-1)) and their rheograms exhibited a non-Newtonian pseudoplastic behavior. The best in vitro drug release control was obtained for HG-CP-NC (1.03±0.11μgcm(-2)h) compared to the HG-CP-NE (1.65±0.19μgcm(-2)h) and the hydrogels containing nonencapsulated drug (HG-CP) (2.79±0.22... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876798 Fri, 13 May 2011 23:00:00 +0100 4876798 http://www.medworm.com/index.php?rid=4876799&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21596136%26dopt%3DAbstract Authors: Kindermann C, Mathée K, Strohmeyer J, Sievert F, Breitkreutz J The aim of the study was the formulation of polyelectrolyte complexes composed of poorly water-soluble acid drugs and basic polymethacrylates by hot-melt extrusion enabling a tailor-made release pattern by the addition of inorganic salts. The influence of different electrolytes was analyzed at varying conditions in order to control drug delivery from the complexes. Poorly water-soluble model drugs naproxen and furosemide were applied in their non-ionic form. After hot-melt extrusion of the naproxen-polymethacrylate powder blend, XRPD and DSC measurements indicated the formation of a single-phase amorphous system. Milled extrudates were stable under storage at long-term and intermediate conditions. Polyelectrolyte ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876799 Tue, 10 May 2011 23:00:00 +0100 4876799 http://www.medworm.com/index.php?rid=4876800&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21596135%26dopt%3DAbstract In conclusion, this paper shows the enhancement of solubility and cell cycle arrest of QCT loaded into micelles composed of mPEG750-b-OCL modified with benzyl end groups. These micelles are therefore considered to be an attractive vehicle for the (targeted) delivery of QCT to tumors. PMID: 21596135 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876800 Mon, 09 May 2011 23:00:00 +0100 4876800 http://www.medworm.com/index.php?rid=4876802&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21575719%26dopt%3DAbstract The objective of the present study was to evaluate the potential of paclitaxel loaded micelles fabricated from PEG(5000)-DSPE as a sustained release system following pulmonary delivery. PEG(5000)-DSPE micelles containing paclitaxel were prepared by solvent evaporation technique followed by investigation of in vitro release of paclitaxel in lung simulated fluid. Tissue distribution and plasma pharmacokinetics of the PEG-lipid micelles after intratracheal and intravenous administrations were investigated in addition to intratracheally administered taxol. Finally, toxicological profile of PEG(5000)-DSPE was investigated. Paclitaxel was successfully formulated in PEG-lipid micelles with encapsulation efficiency of 95%. The PEG-lipid micelles exhibited a sustained release behavior in the simula... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876802 Fri, 06 May 2011 23:00:00 +0100 4876802 http://www.medworm.com/index.php?rid=4876801&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21575720%26dopt%3DAbstract In this study, the phenolic molecules catechol, caffeic acid, and 2,5-dihydroxybenzoic acid were successfully coupled to glucosamine as model substrate in a 1:1 ratio using laccase. Furthermore, coupling of these molecules onto chitosans of different sizes was demonstrated, resulting in decrease in -NH(2) groups as quantified via derivatization. A concomitant increase in iron-chelating capacity from below 3% to up to 70% upon phenolic functionalization was measured for the chitosans based on reduced ferrozine/Fe(2+) complex formation. Interesting these phenolic compounds seems to also participate as cross-linkers in producing characteristic microspheres. This work therefore opens-up new strategies aimed at developing a new generation of iron-chelating biomedical polymers. PMID: 2157572... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876801 Fri, 06 May 2011 23:00:00 +0100 4876801 http://www.medworm.com/index.php?rid=4876804&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21571066%26dopt%3DAbstract In this study, we evaluated F4 and F18 coated with thiolated Eudragit microspheres (TEMS) as a candidate for an oral vaccine. The average particle sizes of TEMS, F4-loaded TEMS, and F18-loaded TEMS were measured as 4.2±0.75μm, 4.7±0.50μm, and 4.5±0.37μm, respectively. F4 is more efficiently encapsulated than F18 in the loading with TEMS. In the release test, F4 and F18 fimbriae were protected in acidic circumstances, whereas most were released at pH 7.4 of intestine circumstances. Production of TNF-α and NO from RAW 264.7cells was increased in a time-dependent manner after exposure to all groups, whereas only F4- or F18-loaded TEMS-stimulated IL-6 secretion. The levels of IFN-γ from mouse splenocytes after exposure to F4 or F18 were increased while IL-4 was not detectable. These re... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876804 Thu, 05 May 2011 23:00:00 +0100 4876804 http://www.medworm.com/index.php?rid=4876806&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21569844%26dopt%3DAbstract The objective of the present study was to develop a novel in vitro system to simulate the process of dissolution and permeation of oral solid dosage forms in vivo, and to establish a correlation between in vitro permeation and in vivo absorption that could predict the bioavailability (BA) and bioequivalence (BE) of congeneric products. The in vitro dissolution and absorption kinetics of four dosage forms of isosorbide mononitrate (ISMN) were evaluated by the USP basket/paddle system and drug dissolution/absorption simulating system (DDASS). The corresponding pharmacokinetic study was performed in beagle dogs. A comparative study was carried out between the classical and the novel method to estimate the effectiveness of the modified DDASS in simulating the course of dissolution and absorpti... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876806 Wed, 04 May 2011 23:00:00 +0100 4876806 http://www.medworm.com/index.php?rid=4876805&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21570466%26dopt%3DAbstract Authors: Bialleck S, Rein H Spherical starch pellets were directly and continuously produced using hot-melt extrusion and die-face pelletisation. In contrast to conventional pelletisation procedures, a discontinuous spheronisation step can be dropped. Pellets were produced based on four different starches (corn starch, pea starch, potato starch and waxy corn starch), four different active ingredients (ibuprofen, paracetamol, phenazon and tramadol-HCl) and various additives. The resulting pellets exhibit a large mechanical stability, low porosity and small surface area. Pellets with a very narrow particle size distribution and particle sizes even in the micron scale can be produced. The drug is either dispersed or dissolved in the starch melt. Drug loadings of up to 80% are achievable. ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876805 Wed, 04 May 2011 23:00:00 +0100 4876805 http://www.medworm.com/index.php?rid=4876803&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21571067%26dopt%3DAbstract We report a systematic investigation of the diuretic bioactivity profiles of phase inversion micronized furosemide and furosemide co-precipitated with Eudragit L100, as well as their blends with stock furosemide, targeted at reducing the rapid spike in diuresis associated with immediate release formulations while maintaining cumulative urine output. Of the formulations tested, an equal parts blend of micronized furosemide and stock furosemide demonstrated optimal diuretic bioactivity profiles in a rat model. PMID: 21571067 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4876803 Wed, 04 May 2011 23:00:00 +0100 4876803 http://www.medworm.com/index.php?rid=4768726&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21527341%26dopt%3DAbstract Authors: Shono Y, Jantratid E, Dressman JB The aim of this study was to evaluate the utility of biorelevant dissolution tests coupled with in silico simulation technology to forecast in vivo bioperformance of poorly water-soluble bases, using nelfinavir mesylate as a model compound. An in silico physiologically based pharmacokinetic (PBPK) model for poorly water-soluble, weakly basic drugs was used to generate plasma profiles of nelfinavir by coupling dissolution results and estimates of precipitation with standard gastrointestinal (GI) parameters and the disposition pharmacokinetics of nelfinavir. In vitro dissolution of nelfinavir mesylate film-coated tablets was measured in biorelevant and compendial media. Drug precipitation in the small intestine was estimated from crystal growth ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4768726 Sun, 17 Apr 2011 23:00:00 +0100 4768726 http://www.medworm.com/index.php?rid=4768725&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21527342%26dopt%3DAbstract Authors: Possidente M, Dragoni S, Franco G, Gori M, Bertelli E, Teodori E, Frosini M, Valoti M ATP-binding cassette (ABC) proteins play key role in tissue defence by transporting metabolic waste and toxic chemicals out of the cells. Consequently, intact cell systems are required to study xenobiotic interactions with ATP-dependent transporters. The aim of the present study was to set up an intestinal precision-cut slice technique to study the interactions of ABC transporters with xenobiotics. Rat intestinal slices were incubated with verapamil, indomethacin and glibenclamide, and the ability of the above-mentioned drugs to inhibit the multidrug resistance glycoprotein (MDR) and/or multidrug-resistance-associated protein (MRP) was assessed by measuring the intracellular conversion of cal... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4768725 Sun, 17 Apr 2011 23:00:00 +0100 4768725 http://www.medworm.com/index.php?rid=4768727&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21515367%26dopt%3DAbstract Authors: Cascone S, De Santis F, Lamberti G, Titomanlio G In this work, a review of the apparatuses available to mimic what happens to a drug (or to foodstuffs) once ingested is presented. Similarly, a brief review of the models proposed to simulate the fate of a drug administered to a living body is reported. Then, the release kinetics of extended release of diclofenac from a commercial enteric-coated tablet was determined both in a conventional dissolution tester (USP Apparatus 2, Method A) as well as in an apparatus modified to reproduce a given pH evolution, closer to the real one than the one suggested by USP. The two experimental release profiles were reported and discussed; therefore, they were adopted as input functions for a previously proposed pharmacokinetic model. The obtai... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4768727 Fri, 15 Apr 2011 23:00:00 +0100 4768727 http://www.medworm.com/index.php?rid=4768728&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21501683%26dopt%3DAbstract Authors: Suñé-Negre JM, Pérez P, Roig M, Fuster R, Hernández C, Ruhí R, García-Montoya E, Miñarro M, Ticó JR As a methodology for characterizing substances in relation to their viability in direct compression, the SeDeM Diagram Expert System may be considered an open system in terms of the number of parameters applied and the optimization of these parameters. With the experience acquired from applying the SeDeM Diagram, in this study, we propose optimizing the parameters corresponding to the Hausner index (IH) and relative humidity (%HR) in order to simplify the mathematical calculation, so that it provides reliable data that can be extrapolated. The proposed optimization does not involve a conceptual change in the parameters considered nor a significant change in the results o... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4768728 Fri, 08 Apr 2011 23:00:00 +0100 4768728 http://www.medworm.com/index.php?rid=4768729&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21496485%26dopt%3DAbstract Authors: Zhang L, Zhu S, Qian L, Pei Y, Qiu Y, Jiang Y This work was based on our recent studies that a promising conjugate, RGD-modified PEGylated polyamidoamine (PAMAM) dendrimer with doxorubicin (DOX) conjugated by acid-sensitive cis-aconityl linkage (RGD-PPCD), could increase tumor targeting by binding with the integrin receptors overexpressed on tumor cells and control release of free DOX in weakly acidic lysosomes. To explore the application of RGD-PPCD to glioma therapy, the effects of the conjugate were further evaluated in glioma model. For comparative studies, DOX was also conjugated to PEG-PAMAM by acid-insensitive succinic linkage to produce the PPSD conjugates, which was further modified by RGD to form RGD-PPSD. In vitro cytotoxicity of the acid-sensitive conjugates agains... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4768729 Thu, 07 Apr 2011 23:00:00 +0100 4768729 http://www.medworm.com/index.php?rid=4543679&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21354513%26dopt%3DAbstract Authors: Lehr CM, Daum N, Schneider M, Schäfer UF PMID: 21354513 [PubMed - in process] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543679 Fri, 04 Mar 2011 04:39:31 +0100 4543679 http://www.medworm.com/index.php?rid=4543671&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21362475%26dopt%3DAbstract Authors: Iqbal J, Sakloetsakun D, Bernkop-Schnürch A The aim of the present study was to investigate the potential of different thiolated polymers (thiomers) on the catalytic activity of CYP450s on one hand and to explore new inhibitors for CYP activity on the other hand. Several thiolated polymers including poly(acrylic acid)-cysteine (PAA-cysteine), chitosan-thioglycolic acid (chitosan-TGA) and thiolated PEG-g-PEI co-polymer along with brij(®) 35, myrj(®) 52 and the well-established CYPP450 inhibitor verapamil were screened for their CYP3A4 and CYP2A6 inhibitory activity and their IC(50) values were determined. Both enzyme inhibition assays were performed in 96-well microtiter plates. 7-Benzyloxy-4-(trifluoromethyl)-coumarin (BFC) and 7-hydroxycoumarin (7-HC) were used as fluoresc... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543671 Sat, 26 Feb 2011 00:00:00 +0100 4543671 http://www.medworm.com/index.php?rid=4543740&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21352913%26dopt%3DAbstract Authors: Kreye F, Siepmann F, Willart JF, Descamps M, Siepmann J The aim of this work was to better understand which physicochemical processes are involved in the control of drug release from lipid implants prepared by melting & casting. Lipid implants gain steadily in importance as controlled parenteral drug delivery systems: In contrast to PLGA-based devices no acidic microclimates are created, which can inactivate incorporated drugs. The melting & casting method offers various advantages over the commonly used direct compression technique. For example, powder de-mixing during manufacturing and highly challenging scale-up due to poor powder flowability are avoided. Importantly, broad spectra of drug release patterns can be easily provided by varying the type of lipid. The res... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543740 Tue, 22 Feb 2011 00:00:00 +0100 4543740 http://www.medworm.com/index.php?rid=4543734&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21352914%26dopt%3DAbstract In conclusion our study demonstrated the efficacy of a novel formulation of baclofen, which exploits the advantages of SLN preparations. However, for clinical purposes, high baclofen concentrations in brain tissue and sedation may be unwanted effects, requiring further studies and optimization of dosages. PMID: 21352914 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543734 Tue, 22 Feb 2011 00:00:00 +0100 4543734 http://www.medworm.com/index.php?rid=4543726&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21352915%26dopt%3DAbstract Authors: Souza LG, Silva EJ, Martins AL, Mota MF, Braga RC, Lima EM, Valadares MC, Taveira SF, Marreto RN Topotecan is an important cytotoxic drug that has gained broad acceptance in clinical use for the treatment of refractory ovarian and small-cell lung cancer. The lactone active form of topotecan can be hydrolyzed in vivo, decreasing the drug's therapeutic efficacy. Lipid encapsulation may promote in vivo stabilization by removing topotecan from aqueous media. Earlier reports of topotecan lipid nanoencapsulation have focused on liposomal encapsulation; however, the higher stability and cost-effectiveness of solid lipid nanoparticles (SLN) highlight the potential of these nanoparticles as an advantageous carrier for topotecan. The initial motivation for this work was to develop, for ... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543726 Tue, 22 Feb 2011 00:00:00 +0100 4543726 http://www.medworm.com/index.php?rid=4543710&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21352916%26dopt%3DAbstract In this study zolmitriptan sublingual tablets were prepared by direct compression method using different mucoadhesive polymers such as hydroxypropyl methyl cellulose, chitosan and sodium carboxy methyl cellulose at a concentration range of 0.5-5% to reduce flushing action of saliva and provide enough time for drug to be absorbed. Tablets were evaluated for the physical properties and optimum formulations were chosen for in vivo studies to carry on sheep model. The tablets disintegrated rapidly and dissolution tests revealed that zolmitriptan was dissolved from the formulation within the compendial limits. This especially showed us that the concentration range of polymers is in acceptable limit. It was also concluded that microcrystalline cellulose, spray dried lactose and sodium starch gly... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543710 Tue, 22 Feb 2011 00:00:00 +0100 4543710 http://www.medworm.com/index.php?rid=4543753&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21349330%26dopt%3DAbstract Authors: Muschert S, Siepmann F, Leclercq B, Siepmann J When using aqueous polymer dispersions for the preparation of controlled release film coatings, instability during long term storage can be a crucial concern. Generally, a thermal after treatment is required to assure sufficient polymer particle coalescence. This curing step is often performed under static conditions in an oven, which is a time-consuming and rather cumbersome process. Dynamic curing in the fluidized bed presents an attractive alternative. However, yet little is known on the required conditions, in particular: temperature, time and relative humidity, to provide stable film structures. The aim of this study was to better understand the importance of these key factors and to evaluate the potential of dynamic curing c... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543753 Mon, 21 Feb 2011 00:00:00 +0100 4543753 http://www.medworm.com/index.php?rid=4543747&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21349331%26dopt%3DAbstract Authors: Lira MC, Santos-Magalhães NS, Nicolas V, Marsaud V, Silva MP, Ponchel G, Vauthier C The aim was to synthesize and characterize fucoidan-coated poly(isobutylcyanoacrylate) nanoparticles. The nanoparticles were prepared by anionic emulsion polymerization (AEP) and by redox radical emulsion polymerization (RREP) of isobutylcyanoacrylate using fucoidan as a new coating material. The nanoparticles were characterized and their cytotoxicity was evaluated in vitro on J774 macrophage and NIH-3T3 fibroblast cell lines. Cellular uptake of labeled nanoparticles was investigated by confocal fluorescence microscopy. Results showed that both methods were suitable to prepare stable formulations of fucoidan coated PIBCA nanoparticles. Stable dispersions of nanoparticles were obtained by AEP w... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543747 Mon, 21 Feb 2011 00:00:00 +0100 4543747 http://www.medworm.com/index.php?rid=4543760&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21345371%26dopt%3DAbstract In this study, we are pioneering new nano-technology for the encapsulation of anticancer drugs (doxorubicin (DOX) and/or docetaxel (DOCE)), whatever their solubility and water affinity. The purpose of this study is to highlight the potential of this recently-patented technology, by carrying out a thorough physicochemical characterisation of these multi-scaled nanocarriers, followed by the study of an encapsulation and release model of hydrophilic anticancer drug. The formulation process is based on a low-energy nano-emulsification method, and allows the generation of a structure composed of oil-based nanocarriers loaded with reverse micelles. Thanks to this, hydrophilic contents can be solubilised in the oily core of this kind of nano-emulsion along with lipophilic content. The results emp... European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543760 Sun, 20 Feb 2011 00:00:00 +0100 4543760 http://www.medworm.com/index.php?rid=4543767&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21333737%26dopt%3DAbstract This study has contributed to improve a fluid bed granulation process, and the process knowledge obtained shows that the product quality can be built in process design, following Quality by Design (QbD) and Process Analytical Technology (PAT) principles. PMID: 21333737 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543767 Thu, 17 Feb 2011 00:00:00 +0100 4543767 http://www.medworm.com/index.php?rid=4543773&cid=s_35550_13_f&fid=35550&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21329757%26dopt%3DAbstract This study demonstrates the potential of substituting FaSSIF with more simple and cost-effective conventional surfactant media. Use of in vivo prognostic amounts of synthetic surfactants in dissolution testing could largely assist in industrial drug development as well as in quality control purposes. PMID: 21329757 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics) European Journal of Pharmaceutics and Biopharmaceutics journals http://www.medworm.com/rss/comments.php?id=4543773 Tue, 15 Feb 2011 00:00:00 +0100 4543773