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European Journal of Pharmaceutical Sciences

Ana Costa, Bruno Sarmento, Vítor Seabra
Mannose receptor is highly expressed on alveolar macrophages, being a potential target to promote the specific local drug delivery of anti-tuberculosis agents through the use of functionalized nanocarriers. In this work, isoniazid (Isn)-loaded solid lipid nanoparticles (SLN), reinforced with stearylamine (SA) were produced by double emulsion technique and further surface-functionalized with mannose in a straightforward chemical approach. Upon pre-formulation assessment, SLN close to 500 nm average size, positively charged and with association efficiency of ISN close to 50% were obtained...
December 8, 2017: European Journal of Pharmaceutical Sciences
Elena Schartmann, Sarah Schemmert, Tamar Ziehm, Leonie H E Leithold, Nan Jiang, Markus Tusche, N Jon Shah, Karl-Josef Langen, Janine Kutzsche, Dieter Willbold, Antje Willuweit
Alzheimer's disease (AD), until now, is an incurable progressive neurodegenerative disease. To target toxic amyloid β oligomers in AD patients' brains and to convert them into non-toxic aggregation-incompetent species, we designed peptides consisting solely of d-enantiomeric amino acid residues. The original lead compound was named D3 and several D3 derivatives were designed to enhance beneficial properties. Here, we compare four d-peptides concerning their efficiency to pass the blood-brain barrier (BBB)...
December 7, 2017: European Journal of Pharmaceutical Sciences
Isara Phiwchai, Wiphawee Yuensook, Natsaree Sawaengsiriphon, Saowalak Krungchanuchat, Chalermchai Pilapong
This report presents the potential utilization of tannic acid (TA) as a natural iron chelator. TA is capable of binding with small ferric complexes without competitive binding with endogenous iron-containing molecules such as ferritin and transferrin. It was observed that the extracellular iron binding of TA resulted in the formation of self-assembled Fe3+-TA complexes, which were then taken up by HepG2 cells via phagocytosis pathway with autophagy-inducing properties. Obviously, TA was found to inhibit iron-induced HepG2 cell growth...
December 7, 2017: European Journal of Pharmaceutical Sciences
Michael Murray, Tina B Gillani, Sussan Ghassabian, Robert J Edwards, Tristan Rawling
The tyrosine kinase inhibitors sorafenib and imatinib are important in the treatment of a range of cancers but adverse effects in some patients necessitate dosage modifications. CYP3A4 has a major role in the oxidation of sorafenib to its N-oxide and N-hydroxymethyl metabolites and also acts in concert with CYP2C8 to mediate imatinib N-demethylation. CYP3A4 expression and function are impaired in patients with advanced liver disease, whereas the functions of CYP2C enzymes are relatively preserved. We evaluated the biotransformation of sorafenib and imatinib in well-characterized microsomal fractions from 17 control subjects and 19 individuals with hepatic cirrhosis of varying severity...
December 6, 2017: European Journal of Pharmaceutical Sciences
Taotao Huo, Chun Tao, Minxin Zhang, Qinghong Liu, Bing Lin, Zhihong Liu, Jialiang Zhang, Meijing Zhang, Haiyue Yang, Jue Wu, Xinrong Sun, Qian Zhang, Hongtao Song
This study aimed to compare the dissolution and the intestinal absorption of tacrolimus in self-microemulsifying drug delivery system (SMEDDS) and solid dispersion (SD). Poloxamer 188 SD was prepared by the combination of the solvent evaporation method and the freeze drying method. Hydroxypropyl methylcellulose (HPMC) SD was prepared by the solvent evaporation method combined with the vacuum drying method. The formation of SD was confirmed by SEM images which showed new solid phases. The SMEDDS was composed of oil (Labrafil M1944 CS 28%), surfactant (Cremophor EL 48%) and co-surfactant (Transcutol P 24%)...
December 5, 2017: European Journal of Pharmaceutical Sciences
Samaneh Pazesh, Ann-Sofie Persson, Jonas Berggren, Göran Alderborn
The purpose of this study was to investigate the effect of degree of disorder of a series of α-lactose monohydrate powders, prepared by milling for different time periods, on the plastic and the elastic stiffness of the particles. As references, a series of physical mixtures consisting of original crystalline particles and amorphous particles obtained by spray-drying was used. In addition, the effect of powder pre-storage humidity on the mechanical properties was investigated. For milled particles of a low degree of disorder, a decreased particle size increased the particle plastic stiffness...
December 4, 2017: European Journal of Pharmaceutical Sciences
Beatriz Martínez-Pérez, David Quintanar-Guerrero, Melina Tapia-Tapia, Ricardo Cisneros-Tamayo, María L Zambrano-Zaragoza, Sergio Alcalá-Alcalá, Néstor Mendoza-Muñoz, Elizabeth Piñón-Segundo
This study aimed to prepare poly (d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) with chitosan (CTS) surface modification to be used as a vaginal delivery system for antimycotic drugs. Clotrimazole was encapsulated with entrapment efficiencies of 86.1 and 68.9% into Clotrimazole-PLGA-NPs (CLT-PLGA-NPs) and PLGA-NPs with CTS-modified surface (CLT-PLGA-CTS-NPs), respectively. The later NPs exhibited a larger size and higher positive zeta potential (Z potential) in comparison to unmodified NPs. In vitro release kinetic studies indicated that Clotrimazole was released in percentages of >98% from both nanoparticulate systems after 18days...
December 2, 2017: European Journal of Pharmaceutical Sciences
P Ronnander, L Simon, H Spilgies, A Koch, S Scherr
In-vitro permeation studies were conducted to assess the feasibility of fabricating dissolving-microneedle-array systems to release sumatriptan succinate. The formulations consisted mainly of the encapsulated active ingredient and a water-soluble biologically compatible polymer, polyvinylpyrrolidone (PVP), approved by the U.S. Food and Drug Administration (FDA). Tests with Franz-type diffusion cells and Göttingen minipig skins showed an increase of the transdermal flux compared to passive diffusion. A preparation, containing 30% by mass of PVP and 8...
December 1, 2017: European Journal of Pharmaceutical Sciences
Frédéric Marçon, Catherine Guittet, Maria A Manso, Ingrid Burton, Luc-André Granier, Philippe Jacqmin, Hervé Dupont
INTRODUCTION: In the absence of a licensed formulation in many countries worldwide, ADV6209, an innovative 2mg/mL oral solution of midazolam containing cyclodextrin, has been developed for moderate sedation in paediatric patients. Population pharmacokinetics for ADV6209 is reported. METHODS: Plasma concentration data were collected from 37 paediatric patients and 12 healthy adults recruited in a single dose, open-label phase II pharmacokinetic study and in a single dose, randomised, open-label two-period crossover bioavailability study, respectively...
December 1, 2017: European Journal of Pharmaceutical Sciences
Yara Santiago de Oliveira, Alcemira Conceição Oliveira, Alejandro Pedro Ayala
Raloxifene hydrochloride is a benzothiophene derivative mainly used in the prevention and treatment of osteoporosis, but exhibits a low bioavailability hindered by its poor water solubility. In this study, a mechanochemical approach based on neat and liquid-assisted grinding was applied to produce new solid forms of raloxifene hydrochloride. The solids obtained were characterized by several solid-state techniques, such as powder X-ray diffraction, thermal analysis, infrared and Raman spectroscopy. These results showed that depending on the processing conditions solvated or amorphous forms can be produced...
November 30, 2017: European Journal of Pharmaceutical Sciences
Yoann Cazaubon, Cédric Mauprivez, Catherine Feliu, Laurent Binet, Olivier Oget, Claire Gozalo, Zoubir Djerada
BACKGROUND AND OBJECTIVES: Articaine is more and more used in third molar surgery under local anesthesia (LA). The objectives of this analysis were to characterize the pharmacokinetics of articaine for this type of surgery and to simulate dosing regimens. METHODS: Non-linear mixed-effects modeling conducted in Monolix 4.4.0 was used to describe articaine plasma concentration-time data from 20 patients. Monte Carlo simulations were then performed to evaluate the probability of cardiotoxic target attainment (PCTA) of various dosage regimens...
November 29, 2017: European Journal of Pharmaceutical Sciences
J Varshosaz, Mohsen Minayian, Ladan Dayyani
Raloxifene HCl (RH) has poor water solubility and due to its extensive first pass metabolism; its bioavailability is only 2%. The purpose of the present study was to enhance the aqueous solubility, oral bioavailability and anti-osteoporotic effects of RH by electro-sprayed nanoparticles (NPs) in ovariectomized rats. NPs containing RH and different ratio of poly(methyl vinyl ether-co-maleic acid) (PMVEMA) were electrosprayed. The voltage, distance of needle to the collector, flow rate of the solution and polymeric percentage were optimized according to the size of NPs and drug solubility...
November 28, 2017: European Journal of Pharmaceutical Sciences
Meenakshi Malhotra, Matt Gooding, James C Evans, Daniel O'Driscoll, Raphael Darcy, Caitriona O'Driscoll
Functional siRNAs (luciferase and PLK1) have been conjugated to β-cyclodextrin and the ability of the conjugates to retain gene knockdown activity has been assessed by delivery to cancer cell lines using various formulations. Initially two formulations used complexation with polycations, namely Lipofectamine 2000 and an amphiphilic polycationic cyclodextrin. Gene knockdown results for human glioblastoma cells (U87) and prostate cancer cells (PC3, DU145) showed that conjugation to the cyclodextrin did not reduce gene silencing by the RNA...
November 27, 2017: European Journal of Pharmaceutical Sciences
Sofieke de Wilde, Maria G H de Jong, Alexander F Lipka, Henk-Jan Guchelaar, Kirsten J M Schimmel
BACKGROUND: Pharmaceutical compounding preparations, produced by (hospital) pharmacies, usually do not have marketing authorization. As a consequence, some of these pharmaceutical compounding preparations can be picked-up by a pharmaceutical company to obtain marketing authorization, often leading to price increases. An example is the 3,4-diaminopyridine slow release (3,4-DAP SR) tablets for Lambert-Eaton Myasthenic Syndrome (LEMS). In 2009 marketing authorization was given for the commercial immediate release phosphate salt of the drug, including a fifty-fold price increase compared to the pharmaceutical compounding preparation...
November 27, 2017: European Journal of Pharmaceutical Sciences
Anjali Pant, Jeetendra Singh Negi
The aim of this study was to develop a novel controlled ionic gelation strategy for chitosan nanoparticle preparation to avoid particle aggregation tendency associated with conventional ionic gelation process. In this study inclusion complexation behaviour of sodium tripolyphosphate (TPP) with beta cyclodextrin (β-CD) has been investigated. The TPP-β-CD inclusion complex was characterized by FT-IR, XRD and DSC techniques. The complexation behaviour was also investigated by molecular docking study. The results showed that the TPP molecule formed inclusion complex with β-CD...
November 27, 2017: European Journal of Pharmaceutical Sciences
A Garcês, M H Amaral, J M Sousa Lobo, A C Silva
Cutaneous use of lipid nanoparticles (solid lipid nanoparticles, SLN and nanostructured lipid carriers, NLC) has been showing promising results. These systems consist of low viscosity aqueous dispersions, being usually employed by means of semi-solid formulations with adequate consistency for skin application. This review addresses the cutaneous use of lipid nanoparticles for therapeutic and cosmetic applications. Initially, general information related to pharmaceutical semi-solid formulations is presented...
November 25, 2017: European Journal of Pharmaceutical Sciences
Joachim Almquist, Daniel Hovdal, Christine Ahlström, Ola Fjellström, Peter Gennemark, Monika Sundqvist
Mathematical models predicting in vivo pharmacodynamic effects from in vitro data can accelerate drug discovery, and reduce costs and animal use. However, data integration and modeling is non-trivial when more than one drug-target receptor is involved in the biological response. We modeled the inhibition of non-esterified fatty-acid release by dual G-protein coupled receptor 81/109A (GPR81/GPR109A) agonists in vivo in the rat, to estimate the in vivo EC50 values for 12 different compounds. We subsequently predicted those potency estimates using EC50 values obtained from concentration-response data in isolated primary adipocytes and cell systems overexpressing GPR81 or GPR109A in vitro...
November 24, 2017: European Journal of Pharmaceutical Sciences
Shinji Kobuchi, Yukiko Yazaki, Yukako Ito, Toshiyuki Sakaeda
Capecitabine, an orally available prodrug of 5-fluorouracil, is widely used to treat patients with colorectal cancer. Although various studies have shown circadian variations in plasma 5-fluorouracil concentrations during long-term infusion, it is still unknown whether circadian variations also exist following administration of capecitabine. The present study aimed to investigate whether the pharmacokinetics of capecitabine and its metabolites, including 5-fluorouracil, vary according to administration time in rats...
November 23, 2017: European Journal of Pharmaceutical Sciences
Lucas Melo da Silveira, Ariadne Botto Fiorot, Thiago Padovani Xavier, Maria Irene Yoshida, Marcelo Antonio de Oliveira
Meloxicam (MLX) is a non-steroidal anti-inflammatory cyclooxygenase (COX) inhibitor that is used to relieve inflammation and pain. MLX has a preferential affinity for COX-2, which is associated with a lower incidence of gastrointestinal side effects. The drug belongs to Class II of the Biopharmaceutical Classification System (BCS) in which dissolution is the limiting step of its bioavailability. In view of this classification, carrying out further studies regarding the compatibility of MLX with excipients and the mechanisms and kinetics of its degradation reactions is fundamental because any changes would directly influence the quality of the product...
November 22, 2017: European Journal of Pharmaceutical Sciences
Hiroaki Shimada, Yuri Kobayashi, Sakiko Tanahashi, Atsushi Kawase, Taro Ogiso, Masahiro Iwaki
Nonsteroidal anti-inflammatory drugs (NSAIDs) can cause idiosyncratic liver injury. Mechanisms involved in NSAID-induced liver injury are complex. Previous studies have suggested that acyl glucuronide of NSAIDs (NSAIDs-Glu) plays an important role in the development of liver injury via covalently binds to proteins and the resultant adduct induces immunological toxicity. As only some NSAIDs-Glu are commercially available, the evaluation of covalent protein adduct formation using ready-made NSAIDs-Glu is difficult and inconvenient...
November 22, 2017: European Journal of Pharmaceutical Sciences
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