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European Journal of Pharmaceutics and Biopharmaceutics

Karin M Rosenblatt, Heike Bunjes
When using lipid nanoparticles as drug carrier system it is important to know how much drug can be loaded to the nanoparticles. The mainly used drug loading procedure is an empirical approach dissolving the drug in the liquid lipid during preparation of the nanoparticles. This approach does not necessarily lead to the truly loadable amount, as the lipid can, e.g. be overloaded, in particular when it is processed in the heat. In this work, a different procedure, passive drug loading, was evaluated to determine the drug loading capacity of various lipid nanoparticles (supercooled trimyristin emulsion droplets, solid trimyristin nanoparticles, tristearin nanoparticles in the α-modification and cholesteryl myristate nanoparticles in the supercooled smectic as well as in the crystalline state)...
March 15, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Laura Schlütke, Markus Immer, Lutz Preu, Frank Totzke, Christoph Schächtele, Michael H G Kubbutat, Conrad Kunick
Rearrangements of anaplastic lymphoma kinase (ALK) are associated with several cancer diseases. Due to resistance development against existing ALK-inhibitors, new, structurally unrelated inhibitors are required. By a scaffold hopping strategy, 6,8-disubstituted purines were designed as analogues of similar ALK-inhibiting thieno[3,2-d]pyrimidines. While the new title compounds indeed inhibited ALK and several ALK mutants in submicromolar concentrations, they retained poor water solubility.
March 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Frédéric Lallemand, Mathieu Schmitt, Jean-Louis Bourges, Robert Gurny, Simon Benita, Jean-Sébastien Garrigue
Local ocular delivery of cyclosporine A (CsA) is the preferred method for CsA delivery as a treatment for ocular inflammatory diseases such as uveitis, corneal healing, vernal keratoconjunctivitis and dry eye disease. However, due to the large molecular weight and hydrophobic nature of CsA and the natural protective mechanisms of the eye, achieving therapeutic levels of CsA in ocular tissues can be difficult. This review gives a comprehensive overview of the current products available to clinicians as well as emerging drug delivery solutions that have been developed at both the academic and industry levels...
March 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Farhath Sultana, Manoj Kumar Neog, MahaboobKhan Rasool
The purpose of the study was to develop a liposomal drug delivery system for morin, a dietary polyphenol, in order to target the synovial macrophages and investigate the remission of disease severity in the adjuvant-induced arthritic (AIA) rats. To do so, mannose decorated liposomal morin (ML-Morin) was prepared using the thin film hydration method and the physicochemical properties were characterized. The particle size and zeta potential of liposomal morin (L-Morin) was found to be 127.9nm ± 2.6 and -24.5mV ± 0...
March 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
John P Gleeson, David J Brayden, Sinéad M Ryan
Ile-Pro-Pro (IPP) and Leu-Lys-Pro (LKP) are food-derived antihypertensive peptides which inhibit angiotensin-converting enzyme (ACE) and may have potential to attenuate hypertension. There is debate over their mechanism of uptake across small intestinal epithelia, but paracellular and PepT1 carrier-mediated uptake are thought to be important routes. The aim of this study was to determine their routes of intestinal permeability using in vitro, ex vivo and in vivo intestinal models. The presence of an apical side pH of 6...
March 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Li Zhang, Xiaoying Xing, Jia Ding, Xiuyun Zhao, Gaofu Qi
Surfactin is a Bacillus-produced natural lipopeptide, which can overcome the epithelial cell barriers for orally delivering insulin, but its ability to promote uptake of insulin by the intestine need to be further improved for a higher oral bioavailability. Here, we designed and synthesized several surfactin variants to improve its ability for oral delivery of insulin. Firstly, we replaced Glu with Gln in surfactin for decreasing its negative charges, but found this replacement weakened its ability to orally delivery insulin...
March 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Toufik Naolou, Eckart Rühl, Andreas Lendlein
No abstract text is available yet for this article.
March 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
J Füller, C C Müller-Goymann
No abstract text is available yet for this article.
March 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Nikhila Miriyala, Defang Ouyang, Yvonne Perrie, Deborah Lowry, Daniel J Kirby
Recent research on porous silica materials as drug carriers for amorphous and controlled drug delivery has shown promising results. However, due to contradictory literature reports on toxicity and high costs of production, it is important to explore alternative safe and inexpensive porous carriers. In this study, the potential of activated carbon (AC) as an amorphous drug carrier was investigated using paracetamol (PA) and ibuprofen (IBU) as model drugs. The solution impregnation method was used for drug loading, with loading efficiency determined by UV spectroscopy and drug release kinetics studied using USP II dissolution apparatus...
March 8, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Nina Hecht, Nils Terveer, Curd Schollmayer, Ulrike Holzgrabe, Lorenz Meinel
Triazolopyrimidine derivatives from the VAS library have been found to be efficient and selective NADPH oxidase (NOX) inhibitors in vitro. In spite of numerous publications on this compound class detailing efficacy for the treatment of cardiovascular diseases, in vivo translation is challenged by their very low water solubility which is preventing further use of these compounds and blocking clinical translation. Therefore, we addressed the challenge of water solubility for three triazolopyrimidine derivatives, VAS2870, VAS3947, and VAS4024, and developed formulations for oral or parenteral application with translational potential into preclinical and clinical studies...
March 8, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Mara Perrone, Angela Lopedota, Elisa Liberati, Vincenzo Russo, Annalisa Cutrignelli, Valentino Laquintana, Irene Pereira de Sousa, Massimo Franco, Serena Tongiani, Nunzio Denora, Andreas Bernkop-Schnürch
The aim of this study was to synthesize, characterize and evaluate the mucoadhesive properties of the first thiolated hyperbranched natural polysaccharide with biodegradability and biocompatibility features. In detail, glycogen-cysteamine conjugates were synthesized through a first step of oxidative ring opening applying increasing concentrations of sodium periodate, to obtain polymers with different degrees of oxidation, and a second step of reductive amination with a constant amount of cysteamine. The obtained glycogen-cysteamine conjugates were characterized regarding their content of free and total thiol groups by Ellman's assay, biocompatibility, swelling/erosion behavior, rheological synergism and mucoadhesive properties in comparison to the unmodified glycogen...
March 5, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Hong Wang, Guangxing Zhang, Xueqin Ma, Yanhua Liu, Jun Feng, Kinam Park, Wenping Wang
Poly (lactide-co-glycolide) (PLGA) microparticles are widely used for controlled drug delivery. Emulsion methods have been commonly used for preparation of PLGA microparticles, but they usually result in low loading capacity, especially for drugs with poor solubility in organic solvents. In the present study, the nanocrystal technology and a water-soluble polymer template method were used to fabricate nanocrystal-loaded microparticles with improved drug loading and encapsulation efficiency for prolonged delivery of breviscapine...
March 2, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Josimar O Eloy, Raquel Petrilli, Deise L Chesca, Fabiano P Saggioro, Robert J Lee, Juliana Maldonado Marchetti
Breast cancer is the second leading cause of cancer deaths among women. Paclitaxel (PTX) is used for its treatment, however non-selectivity, rapid systemic clearance and hypersensitivity to the commercially available formulation are major drawbacks. Rapamycin (RAP), an mTOR inhibitor, acts synergistically with PTX, and thus could be used in combination with it. Drug loading into nanocarriers, particularly liposomes, has proven to enhance efficacy and reduce side-effects of chemotherapeutic drugs. Within this context, the functionalization of liposomes with antibodies for overexpressed receptors on tumor surface is a potential strategy to increase specificity and reduce side-effects...
February 28, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Michele Azzolini, Andrea Mattarei, Martina La Spina, Michele Fanin, Giacomo Chiodarelli, Matteo Romio, Mario Zoratti, Cristina Paradisi, Lucia Biasutto
The biomedical effects of the natural phenol pterostilbene are of great interest but its bioavailability is negatively affected by the phenolic group in position 4' which is an ideal target for the conjugative enzymes of phase II metabolism. We report the synthesis and characterization of prodrugs in which the hydroxyl moiety is reversibly protected as a carbamate ester linked to the N-terminus of a natural amino acid. Prodrugs comprising amino acids with hydrophobic side chains were readily absorbed after intragastric administration to rats...
February 27, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Marius Hittinger, Nicole Schneider-Daum, Claus-Michael Lehr
The interplay of costs and ethics has increased the need for adequate models mimicking the human in vivo situation drastically. An adequate model has the ability to generate data which are predictive for a certain aspect of the human response, for example for the bioavailability. This review highlights how in vitro models can enrich pulmonary drug delivery research with more detailed insights in cellular and non-cellular barriers, allowing for faster improvements and significant innovations of inhalation drug products...
February 27, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Muhammad Irfan, Abid Riaz Ahmed, Andriy Dashevskiy, Karl Kolter, Roland Bodmeier
The objective of this study was to explain curing phenomena for pellets coated with a flexible polymeric coating based on poly(vinyl acetate) (Kollicoat(®) SR 30D) with regard to the effect of starter cores, thickness of drug layer, adhesion of coating to drug-layered-cores as well as coating properties. In addition, appropriate approaches to eliminate the curing effect were identified. Sugar or MCC cores were layered with the model drugs carbamazepine, theophylline, propranolol HCl, tramadol HCl and metoprolol HCl using HPMC (5 or 25% w/w, based on drug) as a binder...
February 25, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Adam Bohr, Yingya Wang, Necati Harmankaya, Jorrit J Water, Stefania Baldursdottír, Kristoffer Almdal, Moritz Beck-Broichsitter
Poly(ethylene carbonate) (PEC) is an unique biomaterial showing significant potential for controlled drug delivery applications. The current study investigated the impact of the molecular weight on the biological performance of drug-loaded PEC films. Following the preparation and thorough physicochemical characterization of diverse PEC (molecular weights: 85, 110, 133, 174 and 196 kDa), the degradation and drug release behavior of rifampicin- and bovine serum albumin-loaded PEC films was investigated in vitro (in the presence and absence of cholesterol esterase), in cell culture (RAW264...
February 23, 2017: European Journal of Pharmaceutics and Biopharmaceutics
C Apfelthaler, M Anzengruber, F Gabor, M Wirth
In the management of bladder cancer, surgical resection of the tumour is usually followed by intravesical instillation of immunomodulatives and/or chemotherapeutics. The purpose of this local intravesical therapy is to eliminate residual malignant cells after surgical intervention. The main limitation of a localised adjuvant therapy is the insufficient concentration of the active pharmaceutical ingredient (API) in malignant cells due to the unique structure of the human urothelium making it an exclusively hard to overcome barrier in the human body...
February 22, 2017: European Journal of Pharmaceutics and Biopharmaceutics
You Jin Jang, Jin Ho Lee, Tae Beom Seo, Se Heang Oh
Local anesthetics are adopted in clinical practice to manage the perioperative and/or postoperative pain. However, their relatively short duration of action limit their ability to meet clinical needs. Herein, we prepared a lidocaine/multivalent ion complex (icLD) using aqueous solutions containing positively charged LD and a multivalent counter-ion as a system for producing prolonged anesthesia. The results of the in vitro and in vivo experiments indicated that the icLD facilitates prolonged LD release even without adjuvants and thus provides nerve blockade for a long duration of action (∼14hrs) without further increase in neurotoxicity than the LD itself...
February 21, 2017: 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
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