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Pharmaceutical Research

Patrick Laurén, Heli Paukkonen, Tiina Lipiäinen, Yujiao Dong, Timo Oksanen, Heikki Räikkönen, Henrik Ehlers, Päivi Laaksonen, Marjo Yliperttula, Timo Laaksonen
PURPOSE: Bioadhesion is an important property of biological membranes, that can be utilized in pharmaceutical and biomedical applications. In this study, we have fabricated mucoadhesive drug releasing films with bio-based, non-toxic and biodegradable polymers that do not require chemical modifications. METHODS: Nanofibrillar cellulose and anionic type nanofibrillar cellulose were used as film forming materials with known mucoadhesive components mucin, pectin and chitosan as functional bioadhesion enhancers...
May 22, 2018: Pharmaceutical Research
Gabriela Wyszogrodzka, Przemysław Dorożyński, Barbara Gil, Wieslaw J Roth, Maciej Strzempek, Bartosz Marszałek, Władysław P Węglarz, Elżbieta Menaszek, Weronika Strzempek, Piotr Kulinowski
PURPOSE: The purpose of the study was initial evaluation of applicability of metal organic framework (MOF) Fe-MIL-101-NH2 as a theranostic carrier of antituberculous drug in terms of its functionality, i.e. drug loading, drug dissolution, magnetic resonance imaging (MRI) contrast and cytotoxic safety. METHODS: Fe-MIL-101-NH2 was characterized using X-ray powder diffraction, FTIR spectrometry and scanning electron microscopy. The particle size analysis was determined using laser diffraction...
May 18, 2018: Pharmaceutical Research
Joanna Zielińska, Jacek Stadnik, Anna Bierczyńska-Krzysik, Dorota Stadnik
PURPOSE: Isolation and identification of unknown impurities of recombinant insulin lispro (produced at IBA) formed during accelerated stability testing of pharmaceutical solutions. For comparative purposes also commercially available formulations of recombinant human insulin (Humulin S®; Lilly), recombinant insulin lispro (Humalog®; Lilly), recombinant insulin aspart (NovoRapid® Penfill®; Novo Nordisk), recombinant insulin detemir (Levemir®; Novo Nordisk) and recombinant insulin glargine (Lantus®; Sanofi-Aventis) were analyzed...
May 16, 2018: Pharmaceutical Research
Sahithi Ravuluri, Rohit Bansal, Nidhi Chhabra, Anurag S Rathore
PURPOSE: To understand non-enzymatic hydrolytic fragmentation of a monoclonal antibody therapeutic under temperature stressed conditions and investigating possible mechanism for the same. METHODS: The mAb therapeutic was incubated at 50°C in phosphate buffer at pH 6.5 and fragmentation was monitored at different ionic strengths under stressed conditions. The incubated mAb was sampled at regular time intervals by analytical Size Exclusion Chromatography (SEC). RESULTS: It was observed that 57% of the mAb product fragmented over 4 days into two fragment species - Fc-Fab and Fab with molecular weights of 97 KDa and 47 KDa, respectively, as measured by mass spectrometry (MS) and sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE)...
May 14, 2018: Pharmaceutical Research
Senpei Yang, Lingyi Li, Tao Chen, Lujia Han, Guoping Lian
PURPOSE: Sebum is an important shunt pathway for transdermal permeation and targeted delivery, but there have been limited studies on its permeation properties. Here we report a measurement and modelling study of solute partition to artificial sebum. METHODS: Equilibrium experiments were carried out for the sebum-water partition coefficients of 23 neutral, cationic and anionic compounds at different pH. RESULTS: Sebum-water partition coefficients not only depend on the hydrophobicity of the chemical but also on pH...
May 14, 2018: Pharmaceutical Research
Issey Takehara, Takashi Yoshikado, Keiko Ishigame, Daiki Mori, Ken-Ichi Furihata, Nobuaki Watanabe, Osamu Ando, Kazuya Maeda, Yuichi Sugiyama, Hiroyuki Kusuhara
PURPOSE: To evaluate association of the dose-dependent effect of rifampicin, an OATP1B inhibitor, on the plasma concentration-time profiles among OATP1B substrates drugs and endogenous substrates. METHODS: Eight healthy volunteers received atorvastatin (1 mg), pitavastatin (0.2 mg), rosuvastatin (0.5 mg), and fluvastatin (2 mg) alone or with rifampicin (300 or 600 mg) in a crossover fashion. The plasma concentrations of these OATP1B probe drugs, total and direct bilirubin, glycochenodeoxycholate-3-sulfate (GCDCA-S), and coproporphyrin I, were determined...
May 10, 2018: Pharmaceutical Research
Ryo Shirakashi, Kiyoshi Takano
PURPOSE: To provide the physicochemical properties of vitrified trehalose for predicting its recrystallization. METHODS: Thin films of vitrified trehalose solutions were prepared at room temperature and exposed to various humid and temperature atmospheres. The in-situ amount of retained water in the vacuum-dried trehalose thin film during exposure was determined using its FTIR spectrum by quantifying the extremely infinitesimal amount of retained water in the trehalose solution...
May 10, 2018: Pharmaceutical Research
Ting Xu, Kajalajit Nahar, Rutesh Dave, Simon Bates, Kenneth Morris
PURPOSE: To study and elucidate the effect of the intensity and duration of processing stresses on the possible solid-state changes during a hot melt extrusion granulation process. METHODS: Blends of α-indomethacin and PEG 3350 (w/w 4:1) were granulated using various screw sizes/designs on the melt extruder under different temperature regimes. Differential Scanning Calorimetry and X-ray Powder Diffraction were employed for characterization. The dissolution behavior of the pure polymorphs and the resulting granules was determined using in-situ fiber optic UV testing system...
May 10, 2018: Pharmaceutical Research
Ryan R Manning, Glenn A Wilson, Ryan E Holcomb, Nathaniel J Zbacnik, Auria A Tellechea, Chelsey L Gilley-Dunn, Ryan J Krammes, Nathan S Krammes, Gabriel J Evans, Charles S Henry, Mark Cornell Manning, Brian M Murphy, Robert W Payne, Derrick S Katayama
PURPOSE: To evaluate the different degrees of residual structure in the unfolded state of interferon-τ using chemical denaturation as a function of temperature by both urea and guanidinium hydrochloride. METHODS: Asymmetrical flow field-flow fractionation (AF4) using both UV and multi-angle laser light scattering (MALLS). Flow Microscopy. All subvisible particle imaging measurements were made using a FlowCAM flow imaging system. RESULTS: The two different denaturants provided different estimates of the conformational stability of the protein when extrapolated back to zero denaturant concentration...
May 9, 2018: Pharmaceutical Research
Yun Yang, Ji Wang, Hongliang He, Wenli Zhang, Yuansheng Zhang, Jianping Liu
PURPOSE: Spherical reconstituted high density lipoprotein (rHDL) can target atherosclerotic lesions by the very low density lipoprotein (VLDL) receptor, which is seldom expressed in liver. By promoting this pathway, the targeting efficiency was hyphothesized to be improved due to avoiding undesired uptake in liver mediated by the scavenger receptor class B type I (SR-BI). In this study, how fatty acid modification in spherical rHDL influenced the VLDL receptor-mediated endocytosis pathway was investigated...
May 7, 2018: Pharmaceutical Research
Lisa-Marie Schaden, Miriam Wimmer-Teubenbacher, Johannes Poms, Peter Laggner, Karl Lohner, Stephan Sacher, Johannes G Khinast, Sharareh Salar-Behzadi
PURPOSE: The effect of different irradiation doses on the structure and activity of lyophilized powders of Hen Egg-White Lysozyme (HEWL) and alcohol dehydrogenase (ADH) was investigated using these substances as models for robust and sensitive proteins, respectively. Three doses were selected to cover the ranges of radio-sterilization (25kGy), treatment of blood products (25Gy) and annual background radiation dose (approximately 2mGy). The results offer an initial screening of different irradiation doses and support the development of X-ray imaging methods as non-destructive process analytical technology (PAT) tools for detecting the visible particulate matters in such products...
May 7, 2018: Pharmaceutical Research
Thibault Vallet, Emilie Belissa, Sandra Laribe-Caget, Alain Chevallier, François-Xavier Chedhomme, Patrick Leglise, Matthieu Piccoli, Hugues Michelon, Vanessa Bloch, Sylvie Meaume, Anne-Sophie Grancher, Nathalie Bachalat, Imad Boulaich, Fattima Abdallah, Maite Rabus, Jean-Paul Rwabihama, Annie-Claude Ribemont, Celia Lachuer, Ines Perquy, Laurent Lechowski, Anne Delahaye, Mathieu Depoisson, Yann Orven, Caroline Guinot, Stephane Gibaud, Corinne Michel, Abdel Mahiou, Sid-Ahmed Belbachir, Jean-Hugues Trouvin, Amelie Dufaÿ-Wojcicki, Vincent Boudy, Fabrice Ruiz
PURPOSE: Medicine acceptability, which is of the utmost importance for vulnerable patients' adherence, is driven by both user and product characteristics. Herein, a novel multivariate approach integrating the many aspects of acceptability is used to discriminate positively and negatively accepted medicines in the older population. METHODS: An observational study was carried out in eight hospitals and eight nursing homes to collect a large set of real-life data on medicines uses in older patients (≥65 years)...
May 7, 2018: Pharmaceutical Research
Jessica J Hung, Barton J Dear, Aileen K Dinin, Ameya U Borwankar, Sumarth K Mehta, Thomas T Truskett, Keith P Johnston
PURPOSE: To explain the effects of the osmolyte proline on the protein-protein interactions (PPI), viscosity and stability of highly concentrated antibody solutions in contrast to other neutral osmolytes. METHODS: The viscosity of ~225 mg/mL mAb solutions was measured with proline, glycine and trehalose as a function of pH and co-solute concentration up to 1.3 M. The stability was assessed via turbidity as well as size exclusion chromatography after 4 weeks storage at 40°C...
April 30, 2018: Pharmaceutical Research
Izabel Almeida Alves, Keli Jaqueline Staudt, Fernando Olinto Carreño, Graziela de Araujo Lock, Carolina de Miranda Silva, Stela Maris Kuze Rates, Teresa Dalla Costa, Bibiana Verlindo De Araujo
PURPOSE: The present work aimed to evaluate the influence of experimental meningitis caused by C. neoformans on total plasma and free brain concentrations of fluconazole (FLC) in Wistar rats. METHOD: The infection was induced by the administration of 100 μL of inoculum (1.105  CFU) through the tail vein. Free drug in the brain was assessed by microdialisys (μD). Blood and μD samples were collected at pre-determined time points up to 12 h after intravenous administration of FLC (20 mg/kg) to healthy and infected rats...
April 27, 2018: Pharmaceutical Research
Woan-Ruoh Lee, Shing-Chuan Shen, Calvin T Sung, Pei-Ying Liu, Jia-You Fang
PURPOSE: Most of the investigations into laser-assisted skin permeation have used the intact skin as the permeation barrier. Whether the laser is effective in improving cutaneous delivery via barrier-defective skin is still unclear. METHODS: In this study, ablative (Er:YAG) and non-ablative (Er:glass) lasers were examined for the penetration of peptide and siRNA upon topical application on in vitro skin with a healthy or disrupted barrier. RESULTS: An enhanced peptide flux (6...
April 26, 2018: Pharmaceutical Research
Andrea Arsiccio, Roberto Pisano
PURPOSE: One of the most common classes of excipients used in protein formulations are buffers. The aim of this work is to investigate the effect of buffers on protein stabilization given by sugars during freeze drying. METHODS: Molecular Dynamics simulations of human growth hormone (hGH) in the presence of sucrose and trehalose were performed, and the impact of phosphate and citrate buffers on their protective action was analyzed. RESULTS: We found that buffers broke the hydrogen bonding network formed by excipients, and the consequences of this disruption of structure ordering were different in sucrose-based or trehalose-based formulations...
April 26, 2018: Pharmaceutical Research
Jean-Baptiste Coty, Magali Noiray, Christine Vauthier
PURPOSE: A Surface Plasmon Resonance chip (SPR) was developed to study the activation of complement system triggered by nanomaterials in contact with human serum, which is an important concern today to warrant safety of nanomedicines. METHODS: The developed chip was tested for its specificity in complex medium and its longevity of use. It was then employed to assess the release of complement fragments upon incubation of nanoparticles in serum. A comparison was made with other current methods assessing complement activation (μC-IE, ELISA)...
April 26, 2018: Pharmaceutical Research
Yue Qiu, Qianwen Yu, Yayuan Liu, Jiajing Tang, Xuhui Wang, Zhengze Lu, Zhuping Xu, Qin He
PURPOSE: Cell penetrating peptides (CPPs) were widely used as motifs for drug delivery to tumor. In former study, an RGD reverse sequence dGR was used to develop active-targeting liposome R8dGR-Lip, which showed well penetrating ability and treatment efficiency on glioma model. However, recurrence after tumor resection caused by post-operative residual cancer cells was a huge obstacle in tumor treatment. In consideration of the effective anti-cancer effect of PTX-R8dGR-Lip when treating glioma in former study, we decide to evaluate its pharmacodynamics on tumor resection models, which were more invasive and resistant...
April 26, 2018: Pharmaceutical Research
Tapan Parikh, Abu T M Serajuddin
PURPOSE: The purpose of this study was to explore the feasibility of developing amorphous solid dispersion (ASD) by inducing acid-base interaction at an elevated temperature using hot melt extrusion. METHODS: Itraconazole and glutaric acid, which do not form salt with each other, were selected as, respectively, model basic drug and weak organic acid. A 1:4:1w/w mixture of itraconazole, glutaric acid and a polymer, Kollidon®VA64, was melt extruded at 95°C. The ground extrudate was characterized by DSC and PXRD and then tested for dissolution at pH 1...
April 25, 2018: Pharmaceutical Research
Pawel Zbyszynski, Bianca R Tomasini-Johansson, Donna M Peters, Glen S Kwon
PURPOSE: To develop PEGylated variants of pUR4/FUD (FUD), a fibronectin assembly inhibitor, using 10 kDa, 20 kDa, and 40 kDa PEGs to evaluate their binding affinity and inhibitory potency. METHODS: The FUD peptide was recombinantly expressed, purified, and PEGylated at the N-terminus using 10 kDa, 20 kDa, and 40 kDa methoxy-PEG aldehyde. The PEGylates were purified and fractionated using ion-exchange chromatography. The molecular weight and degree of PEGylation of each conjugate was verified using MALDI-TOF...
April 24, 2018: Pharmaceutical Research
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