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European Journal of Pharmaceutics and Biopharmaceutics

Kyu-Mok Hwang, Cheol-Hee Cho, Nguyen-Thach Tung, Ju-Young Kim, Yun-Seok Rhee, Eun-Seok Park
This study focuses on developing a highly porous floating tablet containing cilostazol. The underlying release mechanism of cilostazol from porous and floating tablets in dissolution media containing surfactants was investigated. The tablets were prepared by compressing granules and excipients with a sublimating agent, followed by sublimation under vacuum. The volatile material for the sublimating agent was chosen based on its flow properties using conventional methods as well as the twisted blade method. Resultant tablets could float immediately and had significantly higher tensile strengths than conventional tablets of similar porosities, holding a promising potential for increasing gastroretentive properties...
February 20, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Wiebke Kempin, Christian Franz, Lynn-Christine Koster, Felix Schneider, Malte Bogdahn, Werner Weitschies, Anne Seidlitz
The 3D printing technique of fused deposition modeling® (FDM) has lately come into focus as a potential fabrication technique for pharmaceutical dosage forms and medical devices that allows the preparation of delivery systems with nearly any shape. This is particular promising for implants administered at application sites with a high anatomical variability where an individual shape adaption appears reasonable. In this work different polymers (Eudragit®RS, polycaprolactone (PCL), poly(L-lactide) (PLLA) and ethyl cellulose (EC)) were evaluated with respect to their suitability for FDM of drug loaded implants and their drug release behaviour was evaluated...
February 19, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Anna Wrobeln, Julia Laudien, Christoph Groß-Heitfeld, Jürgen Linders, Christian Mayer, Benjamin Wilde, Tanja Knoll, Dominik Naglav, Michael Kirsch, Katja B Ferenz
Until today, artificial oxygen carriers have not been reached satisfactory quality for routine clinical treatments. To bridge this gap, we designed albumin-derived perfluorocarbon-based nanoparticles as novel artificial oxygen carriers and evaluated their physico-chemical and pharmacological performance. Our albumin-derived perfluorocarbon-based nanoparticles (capsules), composed of an albumin shell and a perfluorodecalin core, were synthesized using ultrasonics. Their subsequent analysis by physico-chemical methods such as scanning electron-, laser scanning- and dark field microscopy as well as dynamic light scattering revealed spherically-shaped, nano-sized particles, that were colloidally stable when dispersed in 5% human serum albumin solution...
February 19, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Masatoshi Karashima, Noriyasu Sano, Syunsuke Yamamoto, Yuta Arai, Katsuhiko Yamamoto, Nobuyuki Amano, Yukihiro Ikeda
Micronized cocrystal powders and amorphous spray-dried formulations were prepared and evaluated in vivo and in vitro as pulmonary absorption enhancement formulations of poorly soluble itraconazole (ITZ). ITZ cocrystals with succinic acid (SA) or l-tartaric acid (TA) with a particle size diameter of < 2 µm were successfully micronized using the jet-milling system. The cocrystal crystalline morphologies observed using scanning electron microscopy (SEM) suggested particle shapes that differed from those of the crystalline or spray-dried amorphous ITZ...
February 18, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Anna Cieślak, Nathalie Wauthoz, Alejandro Nieto Orellana, Nolwenn Lautram, Jérôme Béjaud, José Hureaux, Michel Lafleur, Jean-Pierre Benoit, Claudio J Salomon, Guillaume Bastiat
Sterosomes (STEs), a new and promising non-phospholipidic liposome platform based on palmitic acid (PA) and cholesterol (Chol) mixtures, need to have polyethylene glycol (PEG) chains grafted to their surface in order to obtain long-circulating nanocarriers in the blood stream. A post-insertion method was chosen to achieve this modification. The post-insertion process of PEG-modified distearoylphosphoethanolamine (DSPE-PEG) was monitored using the zeta potential value of STEs. Various conditions including PEG chain length and the DSPE-PEG/PA-Chol ratio, were explored...
February 16, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Chara Litou, Maria Vertzoni, Wei Xu, Filippos Kesisoglou, Christos Reppas
PURPOSE: To propose media for simulating the intragastric environment under reduced gastric acid secretion in the fasted state at three levels of simulation of the gastric environment and evaluate their usefulness in evaluating the intragastric dissolution of salts of weak bases. To evaluate the importance of bicarbonate buffer in biorelevant in vitro dissolution testing when using Level II biorelevant media simulating the environment in the fasted upper small intestine, regardless of gastric acid secretions...
February 15, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Robin Meier, Klaus-Peter Moll, Markus Krumme, Peter Kleinebudde
In a previous study a change of the fill-level in the barrel exerted a huge influence on the twin-screw granulation (TSG) process of a high drug loaded, simplified formulation. The present work investigated this influence systematically. The specific feed load (SFL) indicating the mass per revolution as surrogate parameter for the fill-level was applied and the correlation to the real volumetric fill level of an extruder could be demonstrated by a newly developed method. A design of experiments was conducted to examine the combined influence of SFL and screw speed on the process and on critical quality attributes of granules and tablets...
February 15, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Christine Janas, Marc-Philip Mast, Li Kirsamer, Carlo Angioni, Fiona Gao, Werner Mäntele, Jennifer Dressman, Matthias G Wacker
The dispersion releaser (DR) is a dialysis-based setup for the analysis of the drug release from nanosized drug carriers. It is mounted into dissolution apparatus2 of the United States Pharmacopoeia. The present study evaluated the DR technique investigating the drug release of the model compound flurbiprofen from drug solution and from nanoformulations composed of the drug and the polymer materials poly (lactic acid), poly (lactic-co-glycolic acid) or Eudragit(®)RSPO. The drug loaded nanocarriers ranged in size between 185...
February 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Yoo-Seong Jeong, Chang-Soon Yim, Heon-Min Ryu, Chi-Kyoung Noh, Yoo-Kyung Song, Suk-Jae Chung
The objective of the current study was to determine the minimum permeability coefficient, P, needed for perfusion-limited distribution in PBPK. Two expanded kinetic models, containing both permeability and perfusion terms for the rate of tissue distribution, were considered: The resulting equations could be simplified to perfusion-limited distribution depending on tissue permeability. Integration plot analyses were carried out with theophylline in 11 typical tissues to determine their apparent distributional clearances and the model-dependent permeabilities of the tissues...
February 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Justina Vitonyte, Maria Letizia Manca, Carla Caddeo, Donatella Valenti, Josè Esteban Peris, Iris Usach, Amparo Nacher, Maria Matos, Gemma Gutiérrez, Germano Orrù, Xavier Fernàndez-Busquets, Anna Maria Fadda, Maria Manconi
Resveratrol and gallic acid were co-loaded in phospholipid vesicles aiming at protecting the skin from external injuries, such as oxidative stress and microbial infections. Liposomes were prepared using biocompatible phospholipids dispersed in water. To improve vesicle stability and applicability, the phospholipids and the phenols were dispersed in water/propylene glycol or water/glycerol, thus obtaining PEVs and glycerosomes, respectively. The vesicles were characterized by size, morphology, physical stability, and their therapeutic efficacy was investigated in vitro...
February 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Marcela A Moretton, Ezequiel Bernabeu, Estefanía Grotz, Lorena Gonzalez, Marcela Zubillaga, Diego A Chiappetta
Breast cancer represents the top cancer among women, accounting 521.000 deaths per year. Development of targeted nanomedicines to breast cancer tissues represents a milestone to reduce chemotherapy side effects. Taking advantage of the over-expression of glucose (Glu) membrane transporters in breast cancer cells, we aim to expand the potential of a paclitaxel (PTX)-loaded mixed micellar formulation based on polyvinyl caprolactam-polyvinylacetate-polyethylene glycol graft copolymer (Soluplus®) and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) by its surface decoration with Glu moieties...
February 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Shujing Wang, Guoliang Wu, Xinyi Zhang, Zhou Tian, Ning Zhang, Tao Hu, Weiguo Dai, Feng Qian
Surfactants are widely used as stabilizers in the biopharmaceutical formulations to minimize protein aggregation. Under a fixed stress condition, the protecting and destabilizing effects of surfactants are hypothesized to be highly dependent on the species and concentrations of surfactants and mAb. Therefore, we here studied the aggregation-prevention and structure-perturbation effects of eight commonly used surfactants (Tw20, Tw80, Brij35, Chaps, TrX-100, SDS, Pluronic F68 and F127) on two IgG1 solution formulations under agitation, using analytical methodologies including visual inspection, OD350 measurement, HPLC-SEC, circular dicroism, fluorescence spectroscopy and differential scanning calorimetry...
February 9, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Benjamin Balzus, Fitsum Feleke Sahle, Stefan Hönzke, Christian Gerecke, Fabian Schumacher, Sarah Hedtrich, Burkhard Kleuser, Roland Bodmeier
Controlled delivery of corticosteroids using nanoparticles to the skin and corneal epithelium may reduce their side effects and maximize treatment effectiveness. Dexamethasone-loaded ethyl cellulose, Eudragit® RS and ethyl cellulose/Eudragit® RS nanoparticles were prepared by the solvent evaporation method. Dexamethasone release from the polymeric nanoparticles was investigated in vitro using Franz diffusion cells. Drug penetration was also assessed ex vivo using excised human skin. Nanoparticle toxicity was determined by MTT and H2DCFDA assays...
February 9, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Maarten A Mensink, Henderik W Frijlink, Kees van der Voort Maarschalk, Wouter L J Hinrichs
This review aims to provide an overview of current knowledge on stabilization of proteins by sugars in the solid state in relation to stress conditions commonly encountered during drying and storage. First protein degradation mechanisms in the solid state (i.e. physical and chemical degradation routes) and traditional theories regarding protein stabilization (vitrification and water replacement hypotheses) will be briefly discussed. Secondly, refinements to these theories, such as theories focusing on local mobility and protein-sugar packing density, are reviewed in relationship to the traditional theories and their analogies are discussed...
February 9, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Anxo Fernández-Ferreiro, Jesús Silva, Francisco Javier Otero-Espinar, Miguel González-Barcia, María Jesús Lamas, Alvaro Ruibal, Andrea Luaces, Alba Vieites-Prado, Isabel Lema, Michel Herranz, Noemí Gómez-Lado, José Blanco-Mendez, María Gil-Martínez, María Pardo, Alexis Moscoso, Julia Cortes, María Sánchez Martinez, Juan Pardo-Montero, Pablo Aguiar
In last years, sensitive hydrogels have become a breakthrough in ophthalmic pharmaceutical technology aimed at developing new strategies to increase the residence time of active substances. In a previous paper, we qualitatively demonstrated the capacity of a new ion sensitive hydrogel to increase the residence time. Nevertheless, the clearance of the gel from the ocular surface was not quantifiable with the used methodology. The aim of the present work was to use a well-established approach based on scintigraphy to quantitatively estimate the residence time of the previously proposed hydrogel...
February 8, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Aswin Dereymaker, Giulia Cinghia, Guy Van den Mooter
In order to optimize supersaturation levels and avoid early drug precipitation, Eudragit(®) RL was tested as a carrier in solid dispersions, either alone or in combination with a hydrophilic polymer (PVP K25). In vitro dissolution performance of the spray dried solid dispersions was tested. The phase behavior of the produced solid dispersions was analyzed as well as dissolution precipitates. In case of weak acid model compounds (indomethacin and naproxen), the incorporation of Eudragit(®) RL resulted in a prolongation of supersaturation...
February 8, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Ana Rita C Duarte, Ana Sofia D Ferreira, Susana Barreiros, Eurico Cabrita, Rui L Reis, Alexandre Paiva
THEDES, so called therapeutic deep eutectic solvents are here defined as a mixture of two components, which at a particular molar composition become liquid at room temperature and in which one of them is an active pharmaceutical ingredient (API). In this work, THEDES based on menthol complexed with three different APIs, ibuprofen (ibu), BA (BA) and phenylacetic acid (PA), were prepared. The interactions between the components that constitute the THEDES were studied by NMR, confirming that the eutectic system is formed by H-bonds between menthol and the API...
February 8, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Bettina Poller, Clare Strachan, Roland Broadbent, Greg F Walker
The purpose of this study was to evaluate electrospun drug loaded nanofibers as a new matrix for minitablets. Prednisone, a poorly water-soluble drug, was loaded into povidone (polyvinylpyrrolidone, PVP) nanofibers using the process of electrospinning. The drug-loaded nanofiber mat was compressed into minitablets with a 2mm diameter and a height of 2.63±0.04mm. SEM analysis of the minitablet identified a nano-web structure with a nanofiber diameter in the range of 400-500nm. The minitablets met the requirements of the US Pharmacopeia with respect to content uniformity and friability...
February 4, 2017: European Journal of Pharmaceutics and Biopharmaceutics
James I Austerberry, Rana Dajani, Stanislava Panova, Dorota Roberts, Alexander P Golovanov, Alain Pluen, Christopher F van der Walle, Shahid Uddin, Jim Warwicker, Jeremy P Derrick, Robin Curtis
The aggregation propensities of a series of single-chain variable fragment (scFv) proteins harbouring supercharged sequences, salt bridges and lysine/arginine-enriched motifs were characterised as a function of pH and ionic strength to isolate the electrostatic contributions. Recent improvements in aggregation predictors rely on using knowledge of native-state protein-protein interactions. Consistent with previous findings, electrostatic contributions to native protein-protein interactions correlate with aggregate growth pathway and rates...
February 1, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Stefan Grudén, Martin Sandelin, Veera Rasanen, Patrick Micke, Mikael Hedeland, Niklas Axén, Marie Jeansson
BACKGROUND: Docetaxel is a cytostatic agent approved for treatment of non-small cell lung cancer as well as other cancers. Although docetaxel is an effective cytostatic agent, its effectiveness in clinical practice is associated with a variety of acute and long term side-effects. To overcome systemic side effects, a slow release formulation based on calcium sulfate with docetaxel for intra-tumoral administration was developed. METHODS: Two formulations with the calcium sulfate NanoZolid technology were generated with a twofold difference in docetaxel drug load...
February 1, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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