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European Journal of Pharmaceutics and Biopharmaceutics

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https://www.readbyqxmd.com/read/27916704/design-and-development-of-dry-powder-sulfobutylether-%C3%AE-cyclodextrin-complex-for-pulmonary-delivery-of-fisetin
#1
Noratiqah Mohtar, Kevin M G Taylor, Khalid Sheikh, Satyanarayana Somavarapu
This study has investigated complexation of fisetin, a natural flavonoid, with three types of cyclodextrins to improve its solubility. Sulfobutylether-β-cyclodextrin (SBE-β-CD) showed the highest complexation efficiency while maintaining the in vitro antioxidant activity of fisetin. Addition of 20%v/v ethanol in water improved the amount of solubilized fisetin in the complex 5.9-fold compared to the system containing water alone. Spray drying of fisetin-SBE-β-CD complex solution in the presence of ethanol produced a dry powder with improved aerosolization properties when delivered from a dry powder inhaler, indicated by a 2-fold increase in the fine particle fraction (FPF) compared to the powder produced from the complex solution containing water alone...
December 1, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27915005/development-and-characterisation-of-disulfiram-loaded-plga-nanoparticles-for-the-treatment-of-non-small-cell-lung-cancer
#2
Mohammad Najlah, Zahima Ahmed, Mohammed Iqbal, Zhipeng Wang, Patrica Tawari, Weiguang Wang, Christopher McConville
Non-Small Cell Lung Cancer (NSCLC) is the most common type of lung cancer in both men and women. A recent phase IIb study demonstrated that disulfiram (DSF) in combination with cisplatin and vinorelbine was well tolerated and prolonged the survival of patients with newly diagnosed NSCLC. However, DSF is rapidly (4 minutes) metabolised in the bloodstream and it is this issue which is limiting its anticancer application in the clinic. We have recently demonstrated that a low dose of DSF-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles supplemented with oral Cu inhibited tumour growth and reduced metastasis in a xenograft mouse lung cancer model...
November 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27914235/hyaluronan-as-a-promising-excipient-for-ocular-drug-delivery
#3
REVIEW
Michaela Guter, Miriam Breunig
Hyaluronan (HA) is a naturally occurring polysaccharide and well known for its exceptional properties such as high biocompatibility and biodegradability, along with a low immunogenicity. Besides its use for various biomedical applications it recently came into focus as a favorable excipient for the formulation of various ocular therapeutics. This review article summarizes the ocular distribution of HA and its most heavily investigated binding protein "cluster of differentiation 44" (CD44) which is the rationale for the clinical use of HA, primarily as an additive in ocular applications ranging from eye drops to contact lenses...
November 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27914234/food-gastrointestinal-ph-and-models-of-oral-drug-absorption
#4
REVIEW
Ahmad Y Abuhelwa, Desmond B Williams, Richard N Upton, David J R Foster
This article reviews the major physiological and physicochemical principles of the effect of food and gastrointestinal (GI) pH on the absorption and bioavailability of oral drugs, and the various absorption models that are used to describe/predict oral drug absorption. The rate and extent of oral drug absorption is determined by a complex interaction between a drug's physicochemical properties, GI physiologic factors, and the nature of the formulation administered. GI pH is an important factor that can markedly affect oral drug absorption and bioavailability as it may have significant influence on drug dissolution & solubility, drug release, drug stability, and intestinal permeability...
November 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27913127/co-assembly-of-doxorubicin-and-curcumin-targeted-micelles-for-synergistic-delivery-and-improving-anti-tumor-efficacy
#5
Wenzhuan Ma, Qiang Guo, Ying Li, Xiaohui Wang, Jinling Wang, Pengfei Tu
Chemotherapeutic drugs have a series of limitations in anti-tumor treatment, mainly including multidrug resistance (MDR) and serious adverse reactions. Co-delivery system with two or more synergistic therapeutic drugs is an effective strategy to settle these limitations. In this study, active tumor-targeted co-delivery micelles (DOX+Cur)-PMs, with two synergistic drugs of a therapeutic drug of doxorubicin (DOX) and a chemosensitizer of curcumin (Cur) co-encapsulated into hyaluronic acid-vitamin E succinate (HA-VES) graft copolymer, were prepared and delivered simultaneously into tumor cells for improving therapeutic effects of DOX...
November 29, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27903457/glass-forming-ability-of-compounds-in-marketed-amorphous-drug-products
#6
Nicole Wyttenbach, Martin Kuentz
This note is about the glass-forming ability (GFA) of drugs marketed as amorphous solid dispersions or as pure amorphous compounds. A thermoanalytical method was complemented with an in silico study, which made use of molecular properties that were identified earlier as being relevant for GFA. Thus, molar volume together with effective numbers of torsional bonds and hydrogen bonding were used to map drugs that are as amorphous products on the market either as solid dispersion of without co-processed carrier as amorphous drug in a solid dosage form...
November 27, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27903456/millifluidic-synthesis-of-amorphous-drug-polysaccharide-nanoparticle-complex-with-tunable-size-intended-for-supersaturating-drug-delivery-applications
#7
The-Thien Tran, Minh-Hiep Nguyen, Yong Zen Tan, Jia Wei Chew, Saif A Khan, Kunn Hadinoto
The conventional bulk mixing method to prepare amorphous drug-polysaccharide nanoparticle complex (or drug nanoplex in short) has a major drawback in the lack of size control for the nanoplex produced, hence limiting its potential applications as a supersaturating drug delivery system for bioavailability enhancement of poorly soluble drugs. For this reason, we developed a continuous millifluidic synthesis platform of the drug nanoplex exhibiting high size tunability using curcumin (CUR) and chitosan (CHI) as the models for drug and polysaccharides, respectively...
November 27, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27903455/complexation-hydrogels-as-potential-carriers-in-oral-vaccine-delivery-systems
#8
Mia Yoshida, Noriyasu Kamei, Keiya Muto, Jun Kunisawa, Kozo Takayama, Nicholas A Peppas, Mariko Takeda-Morishita
Most current vaccine preparations are in injectable forms, which are inconvenient to patients and ineffective in mucosal immunization. Therefore, most research in this field has been directed at developing ideal oral vaccines enabling the induction of both systemic and mucosal immune responses. In the present study, we examined the utility of a pH-responsive polymeric carrier, poly (methacrylic acid-g-ethylene glycol) [P (MAA-g-EG)] hydrogel, as a potential oral vaccine carrier that can protect cargo proteins in the gastrointestinal tract...
November 26, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27903454/effects-of-frequently-used-pharmaceutical-excipients-on-the-organic-cation-transporters-1-3-and-peptide-transporters-1-2-stably-expressed-in-mdckii-cells
#9
Marcus Otter, Stefan Oswald, Werner Siegmund, Markus Keiser
There is ample evidence that pharmaceutical excipients, which are supposed to be pharmacologically inactive, have an impact on drug metabolism and efflux transport. So far, little is known whether they also modulate uptake transporter proteins. We have recently shown that commonly used solubilizing agents exert significant effects on the function of organic anion uptake transporting polypeptides. Therefore, we investigated in this study the influence of frequently used pharmaceutical excipients on the transport activity of organic cation transporters OCT1, OCT2 and OCT3 and the peptide transporters PEPT1 and PEPT2...
November 26, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27890510/in-situ-forming-pluronic%C3%A2-f127-chitosan-hydrogel-limits-metronidazole-transmucosal-absorption
#10
Sophia Malli, Christian Bories, Bénédicte Pradines, Philippe M Loiseau, Gilles Ponchel, Kawthar Bouchemal
The objective of this work is to design topically-applied thermosensitive and mucoadhesive hydrogel containing metronidazole (MTZ) for the treatment of Trichomonas vaginalis infections. Hydrogel composed of pluronic® F127 (20wt%), chitosan (1wt%) and metronidazole MTZ (0.7wt%) mixture showed its ability to decrease by a factor 4 MTZ flux and apparent permeability absorption through vaginal mucosa. The impact of hydrogel on transmucosal penetration of MTZ was evaluated ex vivo on excised porcine vaginal mucosa mounted on Franz diffusion cell...
November 24, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27890509/small-scale-screening-method-for-low-viscosity-antibody-solutions-using-small-angle-x-ray-scattering
#11
Masakazu Fukuda, Atsushi Watanabe, Akira Hayasaka, Masaru Muraoka, Yuji Hori, Tadao Yamazaki, Yoshimi Imaeda, Akiko Koga
In this study, we investigated the concentration range in which self-association starts to form in humanized IgG monoclonal antibody (mAb) solutions. Furthermore, on the basis of the results, we developed a practical method of screening for low-viscosity antibody solutions by using small-angle X-ray scattering (SAXS) measurements utilizing small quantities of samples. With lower-viscosity mAb3, self-association was not detected in the range of 1-80 mg/mL. With higher-viscosity mAb1, on the other hand, self-association was detected in the range of 10-20 mg/mL and was clearly enhanced by a decrease in temperature...
November 24, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27889415/controlled-extended-octenidine-release-from-a-bacterial-nanocellulose-poloxamer-hybrid-system
#12
Y Alkhatib, M Dewaldt, S Moritz, R Nitzsche, D Kralisch, D Fischer
Although bacterial nanocellulose (BNC) has been widely investigated in the last 10years as drug delivery system, up to now no long-term controlled release of drugs could be realized. Therefore, the aim of the present work was the development of a BNC-based drug delivery system that provides prolonged retention time for the antiseptic octenidine up to one week with improved mechanical and antimicrobial properties as well as a high biocompatibility. BNC was modified by incorporation of differently concentrated Poloxamers 338 and 407 as micelles and gels that were extensively investigated regarding size, surface charge, and dynamic viscosity...
November 24, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27890573/pegylated-oleic-acid-a-promising-amphiphilic-polymer-for-nano-antibiotic-delivery
#13
Calvin A Omolo, Rahul S Kalhapure, Mahantesh Jadhav, Sanjeev Rambharose, Chunderika Mocktar, Valence M K Ndesendo, Thirumala Govender
Vancomycin (VM), a last resort to control methicillin-resistant S. aureus (MRSA) infections, is on the verge of becoming ineffective. Novel nano delivery systems of VM have the potential to combat MRSA. The search for novel materials for nanoantibiotic development is therefore an active research area. In this study, oleic acid (OA) was coupled with monomethoxy polyethylene glycol (mPEG) to obtain a novel bio-safe amphiphilic polymer, mPEG-OA. The critical micelle concentration of mPEG-OA, was found to be 4...
November 23, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27890572/preservative-loss-from-silicone-tubing-during-filling-processes
#14
Verena Saller, Julia Matilainen, Christian Rothkopf, Daniel Serafin, Karoline Bechtold-Peters, Hanns-Christian Mahler, Wolfgang Friess
Significant loss of preservative was observed during filling of drug products during filling line stops. This study evaluated the losses of three commonly used preservatives in protein drugs, i.e. benzyl alcohol, phenol, and m-cresol. Concentration losses during static incubation were quantified and interpreted with regard to the potential driving forces for the underlying sorption, diffusion, and desorption steps. Partitioning from the solution into the silicone polymer was identified as the most decisive parameter for the extent of preservative loss...
November 23, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27890571/facile-fabrication-of-poly-acrylic-acid-coated-chitosan-nanoparticles-with-improved-stability-in-biological-environments
#15
Yukun Wu, Jing Wu, Jing Cao, Yajie Zhang, Zhe Xu, Xiuyi Qin, Wei Wang, Zhi Yuan
Chitosan is one of the most important and commonly used natural polysaccharides in drug delivery for its biocompatible and biodegradable properties. However, poor blood circulation of the chitosan nanoparticles due to their cationic nature is one of the major bottlenecks of chitosan-based drug delivery systems. To address this problem, a versatile platform based on poly(acrylic acid) (PAA) coated ionically cross-linked chitosan/tripolyphosphate nanoparticles (CTS/TPP-PAA NPs), is reported. The zeta potentials of CTS/TPP and CTS/TPP-PAA NPs are approximately 33 mV and -25 mV, respectively...
November 23, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27888144/calcifediol-loaded-liposomes-for-local-treatment-of-pulmonary-bacterial-infections
#16
Arianna Castoldi, Christian Herr, Julia Niederstraßer, Hagar Ibrahim Labouta, Ana Melero, Sarah Gordon, Nicole Schneider-Daum, Robert Bals, Claus-Michael Lehr
The influence of vitamin D3 and its metabolites calcifediol (25(OH)D) and calcitriol on immune regulation and inflammation is well described, and raises the question of potential benefit against bacterial infections. In the current study, 25(OH)D was encapsulated in liposomes to enable aerosolisation, and tested for the ability to prevent pulmonary infection by Pseudomonas aeruginosa. Prepared 25(OH)D-loaded liposomes were nanosized and monodisperse, with a negative surface charge and a 25(OH)D entrapment efficiency of approximately 23%...
November 22, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27888143/dissolution-behavior-of-co-amorphous-amino-acid-indomethacin-mixtures-the-ability-of-amino-acids-to-stabilize-the-supersaturated-state-of-indomethacin
#17
Rami Ojarinta, Aki T Heikkinen, Elina Sievänen, Riikka Laitinen
Arginine, phenylalanine, and tryptophan have been previously shown to improve the solid-state stability of amorphous indomethacin. The present study investigates the ability of these amino acids to prolong the supersaturation of indomethacin in both aqueous and biorelevant conditions either when freely in solution or when formulated as co-amorphous mixtures. The co-amorphous amino acid-indomethacin mixtures (molar ratio 1:1) and amorphous indomethacin were prepared by cryomilling. Dissolution and precipitation tests were performed in buffer solutions (pH 5 and 6...
November 22, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27876599/self-emulsifying-drug-delivery-systems-sedds-proof-of-concept-how-to-make-them-mucoadhesive
#18
Gintare Leonaviciute, Nada Trivic Adamovic, Hung Thanh Lam, Julia Rohrer, Alexandra Partenhauser, Andreas Bernkop-Schnürch
AIM: The objective of this study was to provide a proof-of-concept that self-emulsifying drug delivery systems can be made mucoadhesive by the incorporation of hydrophobic mucoadhesive polymers. METHODS: In order to obtain such a hydrophobic mucoadhesive polymer, Eudragit® S100 was thiolated by covalent attachment of cysteamine. After determination of the thiol group content, in vitro mucoadhesion studies (rotating cylinder and rheological measurements) were performed...
November 19, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27870930/influence-of-membrane-material-on-the-production-of-colloidal-emulsions-by-premix-membrane-emulsification
#19
Sandra Gehrmann, Heike Bunjes
Premix membrane emulsification is a possibility to produce colloidal emulsions as carrier systems for poorly water soluble drugs. During the extrusion of a coarse pre-emulsion through a porous membrane, the emulsion droplets are disrupted into smaller droplets. The influence of the membrane material on the emulsification success was investigated in dependence on the emulsifier. Premixed medium chain triglyceride (MCT) emulsions stabilized with five different emulsifiers were extruded through seven different hydrophilic polymeric membrane materials with pore sizes of 200nm...
November 18, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27867113/glycosylation-and-antiproliferative-activity-of-hyperglycosylated-ifn-%C3%AE-2-potentiate-hek293-cells-as-biofactories
#20
Agustina Gugliotta, Natalia Ceaglio, Brenda Raud, Guillermina Forno, Laura Mauro, Ricardo Kratje, Marcos Oggero
Both CHO and HEK cells are interesting hosts for the production of biotherapeutics due to their ability to introduce post-translational modifications such as glycosylation. Even though oligosaccharide structures attached to proteins are conserved among eukaryotes, many differences have been found between therapeutic glycoproteins expressed in hamster and human derived cells. In this work, a hyperglycosylated IFN-α2b mutein (IFN4N) was produced in CHO and HEK cell lines and an extensive characterization of their properties was performed...
November 17, 2016: European Journal of Pharmaceutics and Biopharmaceutics
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