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European Journal of Pharmaceutical Sciences

Ana Topete, Andreia S Oliveira, A Fernandes, T G Nunes, A P Serro, B Saramago
Although the possibility of using drug-loaded ophthalmic lens to promote sustained drug release has been thoroughly pursued, there are still problems to be solved associated to the different alternatives. In this work, we went back to the traditional method of drug loading by soaking in the drug solution and tried to optimize the release profiles by changing the temperature and the time of loading. Two materials commercially available under the names of CI26Y and Definitive 50 were chosen. CI26Y is used for intraocular lenses (IOLs) and Definitive 50 for soft contact lenses (SCLs)...
February 14, 2018: European Journal of Pharmaceutical Sciences
Sanaz Jafarpour Azami, Amir Amani, Hossein Keshavarz, Roqya Najafi-Taher, Mehdi Mohebali, Mohammad Ali Faramarzi, Mahmood Mahmoudi, Saeedeh Shojaee
Treatment of toxoplasmosis is necessary in congenital form and immunocompromised patients. Atovaquone is a powerful suppressor of protozoan parasites with a broad-spectrum activity, but an extremely low water solubility and bioavailability. In this study, nanoemulsion of this drug was prepared with grape seed oil using spontaneous emulsification method to increase bioavailability and efficacy of atovaquone for treatment of toxoplasmosis. In vitro activity of atovaquone nanoemulsion against T. gondii, RH and Tehran strains, was assessed in HeLa cell culture...
February 13, 2018: European Journal of Pharmaceutical Sciences
Jiaqi Zhang, Qingzhong Jia, Jinlong Qi, Hailin Zhang, Yaru Wu, Xiaowei Shi
QO-58 lysine (QO-58L) as a new potassium channel opener, reported to have a potential activity to cure neuropathic pain. The aim of this research is to develop and validate a high-performance liquid chromatography with tandem spectrometry (LC-MS/MS) method for the quantification of QO-58L in rat urine, feces and bile. In addition, analyze and identify the metabolites in urine and bile. The assay for this compound in samples detected with multiple reaction monitoring mode (MRM), and take nimodipine as internal standards (IS)...
February 13, 2018: European Journal of Pharmaceutical Sciences
Luisa Duque, Martin Körber, Roland Bodmeier
The objectives of this study were to prepare lipid-based implants by hot melt extrusion (HME) for the prolonged release of ovalbumin (OVA), and to relate protein release to crystallinity and polymorphic changes of the lipid matrix. Two lipids, glycerol tristearate and hydrogenated palm oil, with different composition and degree of crystallinity were studied. Solid OVA was dispersed within the lipid matrixes and it preserved its stability during extrusion. This was partially attributed to a protective effect of the lipidic matrix...
February 13, 2018: European Journal of Pharmaceutical Sciences
V Mangas-Sanjuan, C Navarro-Fontestad, A García-Arieta, I F Trocóniz, M Bermejo
A semi-physiological two compartment pharmacokinetic model with two active metabolites (primary (PM) and secondary metabolites (SM)) with saturable and non-saturable pre-systemic efflux transporter, intestinal and hepatic metabolism has been developed. The aim of this work is to explore in several scenarios which analyte (parent drug or any of the metabolites) is the most sensitive to changes in drug product performance (i.e. differences in in vivo dissolution) and to make recommendations based on the simulations outcome...
February 13, 2018: European Journal of Pharmaceutical Sciences
Yosuke Hashimoto, Tomoyuki Hata, Minoru Tada, Manami Iida, Akihiro Watari, Yoshiaki Okada, Takefumi Doi, Hiroki Kuniyasu, Kiyohito Yagi, Masuo Kondoh
Claudin-2 (CLDN-2), a pore-forming tight-junction protein with a tetra-transmembrane domain, is involved in carcinogenesis and the metastasis of some cancers. Although CLDN-2 is highly expressed in the tight junctions of the liver and kidney, whether CLDN-2 is a safe target for cancer therapy remains unknown. We recently generated a rat monoclonal antibody (mAb, clone 1A2) that recognizes the extracellular domains of human and mouse CLDN-2. Here, we investigated the safety of CLDN-2-targeted cancer therapy by using 1A2 as a model therapeutic antibody...
February 12, 2018: European Journal of Pharmaceutical Sciences
Debbie Grønlund, Jakob L Poulsen, Klaus Krogh, Christina Brock, Donghua Liao, Hans Gregersen, Asbjørn M Drewes, Anne E Olesen
BACKGROUND AND AIMS: Opioid treatment interferes with anal sphincter function and its regulation during defecation. This may result in straining, incomplete evacuation, and contribute to opioid-induced bowel dysfunction (OIBD). Employing an experimental model of oxycodone-induced OIBD, we hypothesized that co-administration of the peripherally acting μ-opioid antagonist naloxegol would improve anal sphincter function in comparison to placebo. METHODS: In a double-blind randomized crossover trial, 24 healthy males were assigned to a six-day treatment of oral oxycodone 15 mg twice daily in combination with either oral naloxegol 25 mg once daily or placebo...
February 9, 2018: European Journal of Pharmaceutical Sciences
Shubhajit Paul, Changquan Calvin Sun
As an essential formulation component for large-scale tablet manufacturing, the lubricant preserves tooling by reducing die-wall friction. Unfortunately, lubrication also often results in adverse effects on tablet characteristics, such as prolonged disintegration, slowed dissolution, and reduced mechanical strength. Therefore, the choice of lubricant and its optimal concentration in a tablet formulation is a critical decision in tablet formulation development to attain low die-wall friction while minimizing negative impact on other tablet properties...
February 9, 2018: European Journal of Pharmaceutical Sciences
Magnus Edinger, Matthias Manne Knopp, Hugo Kerdoncuff, Jukka Rantanen, Thomas Rades, Korbinian Löbmann
In this study, the influence of drug load on the microwave-induced amorphization of celecoxib (CCX) in polyvinylpyrrolidone (PVP) tablets was investigated using quantitative transmission Raman spectroscopy. A design of experiments (DoE) setup was applied for developing the quantitative model using two factors: drug load (10, 30, and 50% w/w) and amorphous fraction (0, 25, 50, 75 and 100%). The data was modeled using partial least-squares (PLS) regression and resulted in a robust model with a root mean-square error of prediction of 2...
February 8, 2018: European Journal of Pharmaceutical Sciences
Hiromasa Uchiyama, Satoshi Nogami, Kotomi Katayama, Keita Hayashi, Kazunori Kadota, Yuichi Tozuka
Curcumin (CUR) solutions prepared with α-glucosyl stevia (Stevia-G) and polyvinylpyrrolidone K-30 (PVP) by evaporation method showed 11,000-fold higher solubility compared to CUR alone. Tri-component formulations of CUR/Stevia-G/PVP in aqueous solution showed improved CUR stability for precipitation-triggering conditions of CUR, such as aqueous dilution and temperature changes. Fluorescence study with CUR and pyrene indicated that Stevia-G/PVP mixed solutions produce a more hydrophilic microenvironment around their molecules with increasing PVP concentration compared to Stevia-G solution alone...
February 8, 2018: European Journal of Pharmaceutical Sciences
Joana Bicker, Gilberto Alves, Ana Fortuna, Patrício Soares-da-Silva, Amílcar Falcão
Inhibition of the biosynthesis of noradrenaline is a currently explored strategy for the treatment of hypertension, congestive heart failure and pulmonary arterial hypertension. While some dopamine β-hydroxylase (DBH) inhibitors cross the blood-brain barrier (BBB) and cause central as well as peripheral effects (nepicastat), others have limited access to the brain (etamicastat, zamicastat). In this context, peripheral selectivity is clinically advantageous, in order to prevent alterations of noradrenaline levels in the CNS and the occurrence of adverse central effects...
February 8, 2018: European Journal of Pharmaceutical Sciences
Chenzhong Fei, Rufeng She, Guiyu Li, Lifang Zhang, Wushun Fan, Suhan Xia, Feiqun Xue
Tenvermectin (TVM) is a novel 16-membered macrocyclic lactone antibiotics, which contains component TVM A and TVM B. However there is not any report on safety and clinical efficacy of TVM for developing as a potential drug. In order to understand the part of safety and clinical efficacy of TVM, we conducted the acute toxicity test, the standard bacterial reverse mutation (Ames) test and the clinical deworming test. In the acute toxicity studies, TVM, TVM A and ivermectin (IVM) were administrated once by oral gavage to mice and rats...
February 7, 2018: European Journal of Pharmaceutical Sciences
Camille Taccola, Sylvaine Cartot-Cotton, Delphine Valente, Pascal Barneoud, Catherine Aubert, Valérie Boutet, Fabienne Gallen, Murielle Lochus, Sophie Nicolic, Agnès Dodacki, Maria Smirnova, Salvatore Cisternino, Xavier Declèves, Fanchon Bourasset
Efficacy of drugs aimed at treating central nervous system (CNS) disorders rely partly on their ability to cross the cerebral endothelium, also called the blood-brain barrier (BBB), which constitutes the main interface modulating exchanges of compounds between the brain and blood. In this work, we used both, conventional pharmacokinetics (PK) approach and in situ brain perfusion technique to study the blood and brain PK of PKRinh, an inhibitor of the double-stranded RNA-dependent protein kinase (PKR) activation, in mice...
February 7, 2018: European Journal of Pharmaceutical Sciences
Tomás Zambrano, Rosario D C Hirata, Mario H Hirata, Álvaro Cerda, Luis A Salazar
AIM: Although statins are considered a cornerstone for the treatment of high cholesterol levels due to their powerful cholesterol-lowering effects, response to drug administration is still one of the main pitfalls of statin treatment. So far, the reasons underlying this undesired outcome are still poorly understood, but recently, various studies have suggested that miRNAs may be involved. Therefore, we aimed at evaluating the effect of short-term low-dose treatment with 2 statins on miRNAs expression in patients with hypercholesterolemia...
February 7, 2018: European Journal of Pharmaceutical Sciences
Marzena Dworacka, Galina Chukanova, Saule Iskakova, Yergen Kurmambayev, Anna Wesołowska, Bartosz A Frycz, Paweł P Jagodziński, Grzegorz Dworacki
PURPOSE: Alpha-lipoic acid (ALA), widely known as an antioxidant, modifies also serum levels of angiogenic factors in type 2 diabetic patients. These pharmacological activities may influence the status of the cardiovascular system. Taking into consideration that diabetes is related to the increased cardiovascular risk we investigated several effects of ALA on angiogenic factors in the myocardium and in the aortal wall using a rat model of type 2 diabetes. METHODS: Diabetes was induced in Wistar rats by a fat-rich diet and by intraperitoneal injection of a small dose of streptozotocin (30 mg/kg)...
February 7, 2018: European Journal of Pharmaceutical Sciences
Panos Macheras, Athanassios Iliadis, Georgia Melagraki
The aim of this work is to develop a gastrointestinal (GI) drug absorption model based on a reaction limited model of dissolution and consider its impact on the biopharmaceutic classification of drugs. Estimates for the fraction of dose absorbed as a function of dose, solubility, reaction/dissolution rate constant and the stoichiometry of drug-GI fluids reaction/dissolution were derived by numerical solution of the model equations. The undissolved drug dose and the reaction/dissolution rate constant drive the dissolution rate and determine the extent of absorption when high-constant drug permeability throughout the gastrointestinal tract is assumed...
February 6, 2018: European Journal of Pharmaceutical Sciences
SoHyun Bae, Ronilda D'Cunha, Jie Shao, Guohua An
Tyrosine kinase inhibitors (TKI) are a novel and target-specific class of anticancer drugs. One drawback of TKI therapy is cancer resistance to TKI. An important TKI resistance mechanism is enhanced efflux of TKI by efflux transporters, such as Breast Cancer Resistance Protein (BCRP), in cancer cells. 5,7-Dimethoxyflavone (5,7-DMF) is a natural flavonoid which was recently reported to be a potent BCRP inhibitor. In the current study, the effect of 5,7-DMF on the disposition of sorafenib, a TKI which is a good substrate of BCRP, was investigated both in vitro in efflux transporter expressing cells and in vivo in mice...
February 6, 2018: European Journal of Pharmaceutical Sciences
Parameswara Rao Vuddanda, Mustafa Alomari, Cornelius C Dodoo, Sarah J Trenfield, Sitaram Velaga, Abdul W Basit, Simon Gaisford
Warfarin is a widely used anticoagulant that is critical in reducing patient morbidity and mortality associated with thromboembolic disorders. However, its narrow therapeutic index and large inter-individual variability can lead to complex dosage regimes. Formulating warfarin as an orodispersible film (ODF) using thermal ink-jet (TIJ) printing could enable personalisation of therapy to simplify administration. Commercial TIJ printers are currently unsuitable for printing the milligram dosages, typically required for warfarin therapy...
February 4, 2018: European Journal of Pharmaceutical Sciences
Diego Romano Perinelli, Laura Fagioli, Raffaella Campana, Jenny K W Lam, Wally Baffone, Giovanni Filippo Palmieri, Luca Casettari, Giulia Bonacucina
Chitosan is a biodegradable and biocompatible natural polysaccharide that has a wide range of applications in the field of pharmaceutics, biomedical, chemical, cosmetics, textile and food industry. One of the interesting characteristics of chitosan is its antibacterial and antifungal activity, and together with its excellent safety profile in human, it has attracted considerable attention in various research disciplines. The antimicrobial activity of chitosan is dependent on a number of factors, including its molecular weight, degree of deacetylation, degree of substitution, physical form, as well as the structural properties of the cell walls of the target microorganisms...
February 3, 2018: European Journal of Pharmaceutical Sciences
A J P van Heugten, W de Boer, W S de Vries, R J Pieters, H Vromans
Corticosteroids are widely used in topical formulations such as creams (aqueous) and ointments (non-aqueous). The generally used corticosteroids show large molecular resemblance, where especially the 20-keto-21-hydroxyl group bound to the 17 carbon is important for their chemical stability. Oxidation in both aqueous and non-aqueous environment occurs for triamcinolone acetonide (TCA), hydrocortisone (HC) and desoximethasone (DS). Besides the 20-keto-21-hydroxyl group, TCA, HC and DS have different other moieties attached to the same C17...
February 3, 2018: European Journal of Pharmaceutical Sciences
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