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European Journal of Pharmaceutical Sciences

Antonio Lopalco, Alessandra Curci, Angela Lopedota, Annalisa Cutrignelli, Valentino Laquintana, Massimo Franco, Nunzio Denora
The purpose of this study was to develop liquid and solid paediatric formulations of sodium dichloroacetate (DCA) for the treatment of congenital lactic acidosis (CLA). In this work preformulation studies on the active molecule were performed to identify those physico-chemical properties of the drug relevant to the design of the dosage forms and their process of manufacture. TGA and DSC analysis suggested that sodium DCA was very hygroscopic. HPLC and NMR analysis showed that the compound was widely stable in aqueous solutions at 25 and 40 °C at all the pH values studied...
November 14, 2018: European Journal of Pharmaceutical Sciences
Pernille Kjærgaard Qwist, Camilla Sander, Fridolin Okkels, Vibeke Jessen, Stefania Baldursdottir, Jukka Rantanen
The rheological profile of a semi-solid product is a critical quality attribute. To monitor changes of this attribute during manufacturing, it would be beneficial to measure the rheological parameters in an on-line or in-line mode and implement this as a part of a control strategy for manufacturing of semi-solids. None of the process analytical technology (PAT) tools for measuring the rheological parameters have yet been widely accepted in the pharmaceutical area, as most of the equipment can only measure viscosity...
November 14, 2018: European Journal of Pharmaceutical Sciences
Elbio Saidman, Ana K Chattah, Leslie Aragón, Matías Sancho, Gerardo Camí, Claudia Garnero, Marcela Longhi
Mebendazole (MBZ), designated as a WHO essential drug, can exist in diverse solid forms and presents low absorption at the gastrointestinal level. Considering the potential of cyclodextrins to enhance the solubility and permeability of drugs, inclusion complexes of polymorphs A and C of MBZ with β‑cyclodextrin were obtained. The characterization of the complexes in solid state was performed by using a combination of experimental techniques including Fourier transform infrared spectroscopy, powder X-ray diffractometry and solid state nuclear magnetic resonance...
November 13, 2018: European Journal of Pharmaceutical Sciences
Anne Mette Handler, Eva Marxen, Jette Jacobsen, Christian Janfelt
The aim of the study was to visualize the penetration modifying effect of laurocapram on the delivery of diazepam and codeine across buccal mucosa by MALDI Mass Spectrometry Imaging (MALDI-MSI). A qualitative ex vivo study was carried out by mounting porcine buccal mucosa in Ussing chamber sliders and applying a pre-treatment of phosphate buffered saline (PBS) or a 50% (v/v) laurocapram:ethanol solution apically before incubation for 1 or 3 h with a 0.1 M diazepam or 0.1 M codeine solution. MALDI-MSI analysis was performed on vertical cryo-sections of porcine buccal mucosa...
November 12, 2018: European Journal of Pharmaceutical Sciences
Rong Shi, Zhangyao Xu, Xining Xu, Jingyi Jin, Yining Zhao, Tianming Wang, Yuanyuan Li, Yueming Ma
Metformin and berberine are often combined for treating diabetes. In the present study, we evaluated the drug-drug pharmacokinetic interaction between metformin and berberine after oral co-administration in vivo and the underlying mechanism. As revealed by comparison with the metformin-only group, berberine significantly decreased the maximum plasma concentration (Cmax ), area under the curve from 0 to 4 h (AUC0-4h ), and urinary and bile excretion, and increased the kidney tissue concentration of metformin in rats...
November 11, 2018: European Journal of Pharmaceutical Sciences
Ahmad Ziaee, Ahmad B Albadarin, Luis Padrela, Tim Femmer, Emmet O'Reilly, Gavin Walker
Spray drying is increasingly becoming recognized as an efficient drying and formulation technique for pharmaceutical and biopharmaceutical processing. It offers significant economic and processing advantages compared to lyophilisation/freeze-drying techniques even though the optimisation of process parameters is often a costly and time-consuming procedure. Spray Drying has primarily been used in formulating small molecule drugs with low solubility however it is increasingly being applied to the processing of large biomolecules and biopharmaceuticals...
November 11, 2018: European Journal of Pharmaceutical Sciences
Estevan Sonego Zimmermann, Carolina de Miranda Silva, Camila Neris, Bruna Gaelzer da Silva Torres, Stephan Schmidt, Teresa Dalla Costa
Ciprofloxacin (CIP) is indicated for clinical treatment of urinary and respiratory tract infections. Poor infection site penetration and consequent insufficient exposure to the antimicrobial agent may be the reason for some therapeutic failures. Ciprofloxacin is reported as a substrate for efflux transporters, such as P-glycoprotein, which could be related to the presence of sub-therapeutic drug concentration at the infection site. In the present work we evaluated CIP pharmacokinetics (PK) in plasma and lung and prostate tissues of Wistar rats after intravenous (i...
November 10, 2018: European Journal of Pharmaceutical Sciences
Meng Zhou, Wenlong Shi, Fenglin Yu, Yifan Zhang, Bei Yu, Jianzhong Tang, Yan Yang, Yadong Huang, Qi Xiang, Qihao Zhang, Ze Yao, Zhijian Su
TGF-β3 , a subtype of transforming growth factor-β (TGF-β), is essential to various biological processes, including endoderm development, organogenesis, epithelial hyperplasia, synthesis of extracellular matrix, and immune response. Essentially, TGF-β3 engages the TGF-β1 /Smad signaling pathway to stimulate mesenchymal lineage cells, inhibit epithelial or neuroectodermal lineage cells, and regulate repair, remodeling, and potential scarring after cutaneous wounding. We have now expressed recombinant human TGF-β3 in Escherichia coli Origami B (DE3), with yield 300 ± 17 mg/L monomeric protein at pilot scale...
November 10, 2018: European Journal of Pharmaceutical Sciences
Pavan K Vaddady, Ashit Trivedi, Chetan Rathi, Dora B Madhura, Jiuyu Liu, Richard E Lee, Bernd Meibohm
Spectinamides are a novel class of antibiotics under development for the treatment of MDR- and XDR-tuberculosis, with 1599 and 1445 as early lead candidates within this group. In order to evaluate and differentiate the pharmacological properties of these compounds and assist in candidate selection and design of optimal dosing regimens in animal models of Mtb infection, time kill curve assessments were performed in a previously established in vitro PK/PD model system. The performed studies and subsequent pharmacometric analysis indicate that the anti-mycobacterial activity of 1599 exhibits concentration-dependent killing whereas 1445 shows time-dependent killing...
November 9, 2018: European Journal of Pharmaceutical Sciences
Linto Thomas, Jianxiang Xue, Jessica A Dominguez Rieg, Timo Rieg
Lithium is one of the mainstays for the treatment of bipolar disorder despite its side effects on the endocrine, neurological, and renal systems. Experimentally, lithium has been used as a measure to determine proximal tubule reabsorption based on the assumption that lithium and sodium transport go in parallel in the proximal tubule. However, the exact mechanism by which lithium is reabsorbed remains elusive. The majority of proximal tubule sodium reabsorption is directly or indirectly mediated by the sodium-hydrogen exchanger 3 (NHE3)...
November 9, 2018: European Journal of Pharmaceutical Sciences
Nilutpal Sharma Bora, Bhaskar Mazumder, Santa Mandal, Pompy Patowary, Danswrang Goyary, Pronobesh Chattopadhyay, Sanjai Kumar Dwivedi
The presence of 40-50% more UV radiation in high altitude areas renders the plethora of sunscreen products available in the market virtually ineffective. In this light of event, four US FDA approved UV filters were combined with melatonin and pumpkin seed oil to produce a broad spectrum sunscreen cream, which is envisaged to provide optimum sunprotection along with enhanced antioxidant activity. The objective of this study is to evaluate the protective effect of the sunscreen cream against UV radiation-induced skin photoaging in adult Wistar albino rats and identify its possible underlying mechanism...
November 9, 2018: European Journal of Pharmaceutical Sciences
Patrick Ball, Emma Thompson, Simon Anderson, Vanessa Gwenin, Chris Gwenin
Directed enzyme prodrug therapy is a chemotherapy strategy that utilises prodrug-activating enzymes to activate prodrugs at the tumour location, thus reducing off-target effects. The most commonly investigated enzyme for use with the CB1954 prodrug is the NfnB nitroreductase from E. coli. Literature states that CB1954 is reduced by NfnB at the 2- or 4-position at a 1:1 ratio; deviation from this ratio has been observed in the literature, but not further investigated. The kinetic parameters for the genetically-modified enzymes; NfnB-his, NfnB-cys and AuNP-NfnB-cys were assessed and HPLC analysis was used to determine the hydroxylamine product ratios formed when reacted with CB1954...
November 8, 2018: European Journal of Pharmaceutical Sciences
Samir A Anuj, Harsukh P Gajera, Darshna G Hirpara, Baljibhai A Golakiya
The increasing drug-resistance pathogens among gram-positive bacterial species are becoming a major health concern nowadays. Over the past few years, the bactericidal efficacy of nano‑silver against some drug-resistant gram-positive bacteria has been established, however further investigation is needed to determine whether nano‑silver could be an option for the treatment of drug-resistant gram-positive microbial infections. The purpose of the present study was to determine the bactericidal efficacy of nano‑silver with its membrane destroying property using drug-resistant Staphylococcus aureus MTCC 3160...
November 7, 2018: European Journal of Pharmaceutical Sciences
Amr Maged, Abdelfattah A Abdelkhalek, Azza A Mahmoud, Salwa Salah, Mohamed M Ammar, Mahmoud M Ghorab
In this study we explored the role of rosuvastatin calcium in skin regeneration as statins play important role in the field of tissue engineering. Chitosan hydrochloride was crosslinked with different weight ratios of collagen, β-glycerolphosphate and carboxymethyl cellulose to produce scaffolds by lyophilization technique. Subsequently, the fabricated scaffolds were examined for their morphology, water absorption capacity, water retention, friability and in-vitro drug release as well as in-vivo studies. The results revealed porous 3-D structured scaffolds with maximum water absorption values-ranging between 396 and 2993%...
November 6, 2018: European Journal of Pharmaceutical Sciences
Ann-Christin Jacobsen, Philipp Alexander Elvang, Annette Bauer-Brandl, Martin Brandl
The current study documents enhanced apparent solubility of the BCS class II drug celecoxib (CXB) when formulated as solid phospholipid dispersion (SPD) with either mono- or diacyl-phospholipids by freeze drying from hydro-alcoholic solvent. The enhanced solubility upon dispersion in buffer or fasted state simulated intestinal fluid (FaSSIF) is interpreted to be due to two effects: (1) amorphization of CXB, inducing supersaturation, which is also observed when CXB is freeze dried in the absence of phospholipids and (2) association of CXB with spontaneously forming colloidal structures, such as vesicles and/or micelles, promoting solubilization...
November 5, 2018: European Journal of Pharmaceutical Sciences
Carlos E Puerto Galvis, Vladimir V Kouznetsov
Inspired by the simple and attractive structure of zanthoxylamide protoalkaloids: armatamide, rubecenamide, lemairamin, rubemamine and zanthosine; isolated from plants of the genus Zanthoxylum. We report the synthesis of a series of 29 substituted N-phenylethyl cinnamamides through the direct amidation of a variety of cinnamic acids with a broad range of phenylethylamines promoted by tris-(2,2,2-trifluoroethyl) borate (B(OCH2 CF3 )3 ) in excellent yields and under mild reaction conditions. Then, the toxicological profile of the prepared compounds was studied through in silico computational methods, analyzing eight toxicity risks (hepatotoxicity, mutagenic, carcinogenicity, tumorigenic, immunotoxicity, cytotoxicity, irritant and reproductive effects) and two toxicity targets (AOFA and PGH1), while the acute toxicity toward zebrafish embryos (96 hpf-LC50 , 50% lethal concentration) was also determined in the present study...
November 2, 2018: European Journal of Pharmaceutical Sciences
Qianwen Wang, Shaohong Peng, Yue Hu, Chun-Ho Wong, Kin Ming Kwan, H Y Edwin Chan, Zhong Zuo
DB213 is an expanded CAG RNA inhibitor targeting polyglutamine diseases. This current study aims to investigate biopharmaceutic characteristics of DB213 as well as its brain uptake and distribution in C57 wild type mice, R6/2 Huntington's disease mice and Sprague-Dawley (SD) rats via intranasal administration. The biopharmaceutic characteristics of DB213 were investigated in vitro using Calu-3/MDCK/HEK293 cell lines and brain slices for its membrane transport, equilibrium dialysis for its plasma protein/brain tissue bindings and liver/brain microsomes incubation for its enzyme kinetics profiles...
November 1, 2018: European Journal of Pharmaceutical Sciences
Daniela Burau, David Petroff, Philipp Simon, Lisa Ehmann, Christine Weiser, Christoph Dorn, Alexander Kratzer, Hermann Wrigge, Charlotte Kloft
The need for pharmacokinetic knowledge about antibiotics directly at the site of infection, typically the interstitial space fluid (ISF) of tissues, is gaining acceptance for effective and safe treatment. One option to acquire such data is the microdialysis technique employing a catheter with a semipermeable membrane inserted directly in the ISF. A prerequisite is catheter calibration, e.g. via retrodialysis, yielding a conversion factor from measured to true ISF concentrations, termed relative recovery. This value can be influenced by various factors...
October 31, 2018: European Journal of Pharmaceutical Sciences
M Volpp, U Holzgrabe
Ephedrine and its diastereomer pseudoephedrine have long been used in therapy and are part of over-the-counter combination drugs against colds or allergies. Nonetheless, there is scarcely any information on their plasma protein binding in literature. Plasma protein binding is an important parameter from a pharmacokinetic and pharmacodynamic point of view and can play a crucial role in therapy. The aim of this study was to determine the extent of plasma protein binding using ultrafiltration and different types of plasma proteins like human (HSA) and bovine serum albumin (BSA) and human serum...
October 31, 2018: European Journal of Pharmaceutical Sciences
Gabriela C Meirelles, Cassiana Mendes, Thiago Caon, Helder F Teixeira, Gilsane von Poser, Gilles Ponchel
The benzopyran HP1, a compound isolated from Hypericum polyanthemum, has demonstrated significant opioid-mediated antinociceptive activity after its oral administration. Despite the pharmacological potential, the poor aqueous solubility limits the oral absorption of this compound. For this reason, HP1 has been alternatively incorporated in lipid-based drug delivery systems. Given that nanoemulsions showed higher antinociceptive action than the free compound in a previous report, in this study, the main objective was to investigate the intestinal transport mechanisms of this system...
October 28, 2018: European Journal of Pharmaceutical Sciences
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