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European Journal of Pharmaceutical Sciences

Yusuke Tanaka, Ayaka Kawakami, Ami Nanimatsu, Misaki Horio, Jumpei Matsuoka, Takami Wada, Satoshi Kasaoka, Hiroshi Yoshikawa
The aim of this study is to evaluate how supersaturation, precipitation, and re-dissolution processes influence the intestinal absorption of cinnarizine (CNZ), a lipophilic weak base, by monitoring its plasma and luminal concentration-time profile, after oral administration as a HCl solution containing fluorescein isothiocyanate dextran (FD-4), a non-absorbable marker. In the in vitro pH shift experiment, the supersaturation stability was significantly lower when the higher-concentration solution of CNZ (pH1...
October 20, 2016: European Journal of Pharmaceutical Sciences
Preeti Pandey, Peter J Cabot, Benjamin Wallwork, Benedict J Panizza, Harendra S Parekh
Mucoadhesive in situ gelling systems (soluble gels) have received considerable attention recently as effective stimuli-transforming vectors for a range of drug delivery applications. Considering this fact, the present work involves systematic formulation development, optimization, functional evaluation and ex vivo performance of thermosensitive soluble gels containing dexamethasone 21-phosphate disodium salt (DXN) as the model therapeutic. A series of in situ gel-forming systems comprising the thermoreversible polymer poloxamer-407 (P407), along with hydroxypropyl methyl cellulose (HPMC) and chitosan were first formulated...
October 19, 2016: European Journal of Pharmaceutical Sciences
Felix Royo, Laura Palomo, Justyna Mleczko, Esperanza Gonzalez, Cristina Alonso, Ibon Martínez, Miriam Pérez-Cormenzana, Azucena Castro, Juan M Falcon-Perez
Hepatocytes are involved in the endogenous and drug metabolism; many of the enzymes involved in those processes are incorporated into extracellular vesicles and secreted into the bloodstream. Liver-damaging conditions modify the molecular cargo of those vesicles significantly. However, no information about the effect of these hepatic vesicles on the extracellular environment is available. Drug-induced liver damage increases the number of circulating extracellular vesicles and affects the release and content of hepatocyte-derived vesicles...
October 19, 2016: European Journal of Pharmaceutical Sciences
M Puhka, M-E Nordberg, S Valkonen, A Rannikko, O Kallioniemi, P Siljander, T Af Hällström
Urinary extracellular vesicles (EVs) are a promising source of biomarkers, which can be obtained in a non-invasive manner. However, the yield of EVs from urine samples may be insufficient for various analyses due to the entrapment of EVs by the Tamm-Horsfall protein (THP) meshwork. Here, we developed a simple dilution protocol to increase the urinary EV yield by disrupting the interaction between THP filaments and EVs with the help of alkaline pH and lowered ionic concentration. The integrity of the EVs and THP was assessed by electron microscopy...
October 19, 2016: European Journal of Pharmaceutical Sciences
Tao Li, Xiufen Chen, Yajun Liu, Lulu Fan, Liqing Lin, Yu Xu, Sijia Chen, Jingwei Shao
Ursolic acid (UA) as a nature product exhibits good anti-cancer activity, low toxicity, and good liver protection features. However, the low-solubility and poor bioavailability restrict its further clinical application. To overcome this problem, a pH-sensitive prodrug delivery system (UA@MSN-UA) that incorporated acid-sensitive linkage between drug and silica-based mesoporous nanosphere (MSN) was successfully designed and synthesized. The physicochemical properties of the UA@MSN-UA nanoparticles were investigated for shape, particle size, zeta potential, nitrogen adsorption-desorption and infrared (IR) spectroscopy...
October 19, 2016: European Journal of Pharmaceutical Sciences
Guoliang Sa, Xuepeng Xiong, Jiangang Ren, Yifang Zhao, Sangang He
Several animal models have been used in studies associated with oral submucous fibrosis (OSF); however, an appropriate model based on the histopathological characteristics of OSF is still needed. This study aimed to provide histological references for selecting a potential model. The expression intensities of collagen type I (Col I), type III (Col III), type IV (Col IV), fibronectin (FN), transforming growth factors β (TGF-β), and connective tissue growth factor (CCN2) in the oral mucosa of the human and six non-human animal species were measured by immunohistochemistry...
October 18, 2016: European Journal of Pharmaceutical Sciences
Zoraida Andreu, Renan Otta Oshiro, Alberto Redruello, Soraya López-Martín, Cristina Gutiérrez-Vázquez, Esperanza Morato, Ana Isabel Marina, Carlos Olivier Gómez, María Yáñez-Mó
Bladder cancer is the second most frequent malignancy of the urinary tract after prostate cancer. Current diagnostic techniques, such as cystoscopy and biopsies are highly invasive and accompanied of undesirable side effects. Moreover, there are no suitable biomarkers for relapse or progression prognosis. We analysed whether the specific composition of microRNAs (miRNAs) and proteins of extracellular vesicles (EVs) that urothelial tumor cells of bladder mucosa release into the urine, could reflect their pathologic condition...
October 14, 2016: European Journal of Pharmaceutical Sciences
Maíra N Pereira, Heidi L Schulte, Natane Duarte, Eliana M Lima, Livia L Sá-Barreto, Tais Gratieri, Guilherme M Gelfuso, Marcilio S S Cunha-Filho
Currently marketed minoxidil formulations present inconveniences that ranges from a grease hard aspect they leave on the hair to more serious adverse reactions as scalp dryness and irritation. In this paper we propose a novel approach for minoxidil sulphate (MXS) delivery based on a solid effervescent formulation. The aim was to investigate whether the particle mechanical movement triggered by effervescence would lead to higher follicle accumulation. Preformulation studies using thermal, spectroscopic and morphological analysis demonstrated the compatibility between effervescent salts and the drug...
October 13, 2016: European Journal of Pharmaceutical Sciences
K Żółtowska, U Piotrowska, E Oledzka, U Luchowska, M Sobczak, A Bocho-Janiszewska
In this study, "predominantly isotactic", disyndiotactic, and atactic polylactides (PLAs) and poly(ε-caprolactone)s (PCLs) were loaded with anticancer agents, epirubicin (EPI) and cyclophosphamide (CYCLOPHO), to investigate their properties as highly controlled delivery devices. It was found that the kinetic release of drugs from the obtained polyester matrices tested in vitro at 37°C and pH7.4 was strongly dependent on average molecular weight (Mn) of the polymers as well as the PLAs' microstructure. EPI and CYCLOPHO were released from various obtained matrices according to the diffusion, diffusion-degradation, and degradation mechanisms in a rather regular and continuous manner...
October 11, 2016: European Journal of Pharmaceutical Sciences
C Aeberhard, C Steuer, C Saxer, A Huber, Z Stanga, S Mühlebach
BACKGROUND: Parenteral antiepileptic drugs are frequently used in critically ill patients for seizure control therapy or prevention. Many of these patients require additional parenteral nutrition (PN). Therefore, a parallel infusion of the frequently used antiepileptic drug levetiracetam (LEV) is interesting in terms of the restricted i.v. lines (e.g., neonates). The potential interactions of the complex PN admixture with the drug product and the appropriate admixing of a drug at effective dosages require physicochemical lab assessments to obtain specific and reliable pharmaceutical documentation for the intended admixing...
October 11, 2016: European Journal of Pharmaceutical Sciences
Roman Štukelj, Karin Schara, Apolonija Bedina-Zavec, Vid Šuštar, Manca Pajnič, Ljubiša Pađen, Judita Lea Krek, Veronika Kralj-Iglič, Anita Mrvar-Brečko, Rado Janša
During harvesting of nanovesicles (NVs) from blood, blood cells and other particles in blood are exposed to mechanical forces which may cause activation of platelets, changes of membrane properties, cell deformation and shedding of membrane fragments. We report on the effect of shear forces imposed upon blood samples during the harvesting process, on the concentration of membrane nanovesicles in isolates from blood. Mathematical models of blood flow through the needle during sampling with vacutubes and with free flow were constructed, starting from the Navier-Stokes formalism...
October 10, 2016: European Journal of Pharmaceutical Sciences
Masateru Miyake, Toshihisa Koga, Satoshi Kondo, Noriaki Yoda, Chie Emoto, Tadashi Mukai, Hajime Toguchi
An adequate evaluation system for drug intestinal absorption is essential in the pharmaceutical industry. Previously, we established a novel prediction system of drug intestinal absorption in humans, using the mini-Ussing chamber equipped with human intestinal tissues. In this system, the TI value was defined as the sum of drug amounts transported to the basal-side component (X(corr)) and drug amounts accumulated in the tissue (T(corr)), which are normalized by AUC of a drug in the apical compartment, as an index for drug absorption...
October 6, 2016: European Journal of Pharmaceutical Sciences
Łukasz Fijałkowski, Kinga Sałat, Adrian Podkowa, Paula Zaręba, Alicja Nowaczyk
The chemical interaction of nine antiepileptic drugs (tiagabine, gabapentin, pregabalin, lamotrigine, zonisamide, valproic acid, valpromide, vigabatrin, progabide) and two endogenous metabolites (4-aminobutanoic acid, 4-hydroxybutanoic acid) with a model of human GABA transporter 1 (hGAT1) is described using the molecular docking method. To establish the role of hGAT1 in chronic pain, tiagabine, a selective hGAT1 inhibitor, was assessed in the in vivo experiments for its antiallodynic properties in two mouse models of neuropathic pain...
October 6, 2016: European Journal of Pharmaceutical Sciences
Sara Pistone, Francisco M Goycoolea, Alix Young, Gro Smistad, Marianne Hiorth
The efficacy of treatments for oral ailments is often challenged by a low residence time of the conventional pharmaceutical formulations in the oral cavity. The residence time in the oral cavity could be improved by using bioadhesive formulations, such as preparations based on polysaccharides. This study describes the formulation and the evaluation of polysaccharide-based nanosystems as drug delivery systems addressed to the oral cavity. Nanoparticles based on chitosan, alginate or pectin were prepared through self-assembly by ionotropic gelation using oppositely charged crosslinkers (tripolyphosphate or zinc)...
October 6, 2016: European Journal of Pharmaceutical Sciences
Carolina Gómez-Gaete, Macarena Retamal, Catalina Chávez, Paulina Bustos, Ricardo Godoy, Pablo Torres-Vergara
Rhein is an active metabolite of the drug diacerein, whose anti-inflammatory properties have been demonstrated in both in vitro and in vivo models. However, the low oral bioavailability of rhein has limited its utility as a potential treatment of osteoarthritis (OA), a chronic inflammatory disease. In order to overcome this limitation, the aim of this work was the development of a drug delivery system intended for intra-articular administration of rhein, based on polymeric biodegradable PLGA microparticles (MPs) loaded with the drug...
October 6, 2016: European Journal of Pharmaceutical Sciences
Laura C Luciani-Giacobbe, María V Ramírez-Rigo, Yamila Garro-Linck, Gustavo A Monti, Ruben H Manzo, María E Olivera
One of the main obstacles to the successful treatment of tuberculosis is the poor and variable oral bioavailability of rifampicin (RIF), which is mainly due to its low hydrophilicity and dissolution rate. The aim of this work was to obtain a hydrophilic new material that allows a very fast dissolution rate of RIF and therefore is potentially useful in the development of oral solid dosage forms. The acid form of carboxymethylcellulose (CMC) was co-processed with RIF by solvent impregnation to obtain CMC-RIF powder, which was characterized by polarized optical microscopy, powder x-ray diffraction, DSC-TGA, hot stage microscopy, (13)C and (15)N solid-state NMR and FT-IR spectroscopy...
October 6, 2016: European Journal of Pharmaceutical Sciences
Natalie Krahn, Maureen Spearman, Markus Meier, July Dorion-Thibaudeau, Matthew McDougall, Trushar R Patel, Gregory De Crescenzo, Yves Durocher, Jörg Stetefeld, Michael Butler
Glycoengineering of mAbs has become common practice in attempts to generate the ideal mAb candidate for a wide range of therapeutic applications. The effects of these glycan modifications on the binding affinity of IgG mAbs for FcγRIIIa and their cytotoxicity is well known. However, little is understood about the effect that these modifications have on binding to the high affinity FcγRI receptor. This study analysed the effect of variable N-glycosylation on a human-llama hybrid mAb (EG2-hFc, 80 kDa) binding to FcγRI including a comparison to a full-sized IgG1 (DP-12, 150 kDa)...
October 6, 2016: European Journal of Pharmaceutical Sciences
Gaurav Chauhan, Vianni Chopra, Amit Tyagi, Goutam Rath, Rakesh K Sharma, Amit K Goyal
Nano-graphene oxide (GO) nanometal composite (specifically nanogold and nanosilver) have shown to be a promising material for anticancer therapeutics. Owing to their high drug loading capacity, photothermal and synergizing effects, it is very important to exploit them for targeted chemo-thermal cancer therapeutics. In this work, gold nanoparticles (AuNPs) were selected as the composite metal, folic acid (FA) was taken as GO surface functionalization moiety for active tumor targeting of model anticancer drug Doxorubicin (Dox)...
October 6, 2016: European Journal of Pharmaceutical Sciences
Ali Akbar Alizadeh, Maryam Hamzeh-Mivehroud, Malak Farajzadeh, Siavoush Dastmalchi
The aim of this study was to identify novel TNF-α blocking peptide(s) using phage display technology. Two novel 7-mer TNF-α binding peptides P51 and P52 with Kd values of 1.47 and 0.51nM were identified. Phage particles displaying P51 and P52 peptides at 0.318nM concentration prevent cytotoxic effect of TNF-α on L929 cells by 8.2% and 16.15%, respectively. Synthesized P51 and P52 peptides also inhibited TNF-α induced cytotoxicity with IC50 values of 25.15±2.18 and 7.08±2.24μM, respectively. The result of RT-PCR also supports the inhibitory activity of the identified peptides, where P51 and P52 significantly inhibit the inductive effect of TNF-α on IκB-α mRNA levels...
October 5, 2016: European Journal of Pharmaceutical Sciences
Selenia Ternullo, Louis de Weerd, Gøril Eide Flaten, Ann Mari Holsæter, Nataša Škalko-Basnet
Development of effective (trans)dermal drug delivery systems requires reliable skin models to evaluate skin drug penetration. The isolated perfused human skin flap remains metabolically active tissue for up to 6h during in vitro perfusion. We introduce the isolated perfused human skin flap as a close-to-in vivo skin penetration model. To validate the model's ability to evaluate skin drug penetration the solutions of a hydrophilic (calcein) and a lipophilic (rhodamine) fluorescence marker were applied. The skin flaps were perfused with modified Krebs-Henseleit buffer (pH7...
October 5, 2016: European Journal of Pharmaceutical Sciences
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