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https://www.readbyqxmd.com/read/28092857/universal-efavirenz-determination-in-transport-study-rat-placenta-perfusion-and-placenta-lysate-by-hplc-uv
#1
Lucie Zelena, Josef Reznicek, Martina Ceckova, Hana Sklenarova
Efavirenz is an antiretroviral drug used in the treatment of HIV-positive patients. A simple, fast and sensitive high-performance liquid chromatography (HPLC) method was developed in order to determine efavirenz in three types of samples provided from pharmacokinetic studies. The analysis took 5min and was performed using a C18 analytical column (Discovery HS C18, 150×4.6mm, particle size of 5μm) in isocratic mode with a mobile phase containing acetonitrile and water (65:35, v/v), a flow rate of 1.6mLmin(-1), a sample volume of 10μL and UV detection at 245nm...
January 11, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28092854/biopharmaceutical-characterization-of-praziquantel-cocrystals-and-cyclodextrin-complexes-prepared-by-grinding
#2
Martina Cugovčan, Jasna Jablan, Jasmina Lovrić, Dominik Cinčić, Nives Galić, Mario Jug
Mechanochemical activation using several different co-grinding additives was applied as a green chemistry approach to improve physiochemical and biopharmaceutical properties of praziquantel (PZQ). Liquid assisted grinding with an equimolar amount of citric acid (CA), malic acid (MA), salicylic acid (SA) and tartaric acid (TA) gained in cocrystal formation, which all showed pH-dependent solubility and dissolution rate. However, the most soluble cocrystal of PZQ with MA was chemically unstable, as seen during the stability testing...
January 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28092269/analysis-of-microtubule-growth-dynamics-arising-from-altered-actin-network-structure-and-contractility-in-breast-tumor-cells
#3
Eleanor Ory, Lekhana Bhandary, Amanda Boggs, Kristi Chakrabarti, Joshua Parker, Wolfgang Losert, Stuart S Martin
The periphery of epithelial cells is shaped by opposing cytoskeletal physical forces generated predominately by two dynamic force generating systems - growing microtubule ends push against the boundary from the cell center, and the actin cortex contracts the attached plasma membrane. Here we investigate how changes to the structure and dynamics of the actin cortex alter the dynamics of microtubules. Current drugs target actin polymerization and contraction to reduce cell division and invasiveness; however, the impacts on microtubule dynamics remain incompletely understood...
January 16, 2017: Physical Biology
https://www.readbyqxmd.com/read/28090777/biodegradable-neuro-compatible-peptide-hydrogel-promotes-neurite-outgrowth-shows-significant-neuroprotection-and-delivers-anti-alzheimer-drug
#4
Anindyasundar Adak, Gaurav Das, Surajit Barman, Saswat Mohapatra, Debmalya Bhunia, Batakrishna Jana, Surajit Ghosh
A novel neuro-compatible peptide based hydrogel has been designed and developed, which contains microtubule stabilizing and neuroprotective short peptide. This hydrogel shows strong three dimensional cross-linked fibrillary networks, which can capture water molecules. Interestingly, this hydrogel serves as excellent biocompatible soft-material for 2D and 3D (neuro-sphere) neuron cell culture and provides stability of key cytoskeleton filaments such as microtubule and actin. Remarkably, it was observed that this hydrogel slowly enzymatically degrades and releases neuroprotective peptide, which promotes neurite outgrowth of neuron cell as well as exhibits excellent neuroprotection against anti-NGF induced toxicity in neuron cells...
January 16, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28090681/excess-of-exercise-increases-the-risk-of-atrial-fibrillation
#5
REVIEW
A Müssigbrodt, A Weber, J Mandrola, Y van Belle, S Richter, M Döring, A Arya, P Sommer, A Bollmann, G Hindricks
An interesting and still not well-understood example for old medical wisdom "Sola dosis facit venenum" is the increased prevalence of atrial fibrillation (AF) in athletes. Numerous studies have shown a fourfold to eightfold increased risk of AF in athletes compared to the normal population. Analysis of the existing data suggests a dose-dependent effect of exercise. Moderate exercise seems to have a protective effect and decreases the risk of AF, whereas excessive exercise seems to increase the risk of AF. The described cases illustrate clinical manifestations within the spectrum of AF in elderly athletes, that is, exercise-induced AF, vagal AF, chronic AF, and atrial flutter...
January 16, 2017: Scandinavian Journal of Medicine & Science in Sports
https://www.readbyqxmd.com/read/28090074/targeting-of-wnt-%C3%AE-catenin-by-anthelmintic-drug-pyrvinium-enhances-sensitivity-of-ovarian-cancer-cells-to-chemotherapy
#6
Chongyuan Zhang, Zhenge Zhang, Shuirong Zhang, Wenrong Wang, Ping Hu
BACKGROUND Aberrant activation of Wnt/β-catenin has been shown to promote ovarian cancer proliferation and chemoresistance. Pyrvinium, an FDA-approved anthelmintic drug, has been identified as a potent Wnt inhibitor. Pyrvinium may sensitize ovarian cancer cells to chemotherapy. MATERIAL AND METHODS The effect of pyrvinium alone and its combination with paclitaxel in ovarian cancer was investigated using an in vitro culture system and in vivo xenograft models. The mechanisms of its action were also analyzed, focusing on the Wnt/β-catenin pathway...
January 16, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28089916/stable-curcumin-loaded-polymeric-micellar-formulation-for-enhancing-cellular-uptake-and-cytotoxicity-to-flt3-overexpressing-eol-1-leukemic-cells
#7
Singkome Tima, Songyot Chadarat Anuchapreeda Ampasavate, Cory Berkland, Siriporn Okonogi
The present study aims to develop a stable polymeric micellar formulation of curcumin (CM) with improved solubility and stability, and that is suitable for clinical applications in leukemia patients. CM-loaded polymeric micelles (CM-micelles) were prepared using poloxamers. The chemical structure of the polymers influenced micellar properties. The best formulation of CM-micelles, namely CM-P407, was obtained from poloxamer 407 at drug to polymer ratio of 1:30 and rehydrated with phosphate buffer solution pH 7...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28089687/stabilizing-effects-for-antibody-formulations-and-safety-profiles-of-cyclodextrin-polypseudorotaxane-hydrogels
#8
Taishi Higashi, Naoko Ohshita, Tatsunori Hirotsu, Yoshihito Yamashita, Keiichi Motoyama, Sawako Koyama, Ruriko Iibuchi, Takayuki Uchida, Shiuhei Mieda, Kenji Handa, Tomoaki Kimoto, Hidetoshi Arima
Antibodies often have poor physicochemical stability during storage and/or transport, which is a serious drawback for the development of antibody-based drugs. In this study, we prepared polypseudorotaxane (PPRX) hydrogels consisting of cyclodextrins (CyDs) and polyethylene glycol (PEG), and evaluated them as stabilizers for commercially available antibody-based drugs. α-CyD and γ-CyD formed PPRX hydrogels with PEG (MW 20,000 Da) in the presence of antibody-based drugs such as omalizumab, palivizumab, panitumumab, and ranibizumab...
January 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28089660/characterization-pharmacokinetics-and-tissue-distribution-of-chlorogenic-acid-loaded-self-microemulsifying-drug-delivery-system
#9
Li Chen, Chang-Shun Liu, Qing-Zhen Chen, Sen Wang, Yong-Ai Xiong, Jing Jing, Jia-Jia Lv
The purpose of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to improve the oral bioavailability of Chlorogenic acid (CA), an important bioactive compound from Lonicerae Japonicae Flos with poor permeability. SMEDDS was prepared and characterized by self-emulsifying rate, morphological observation, droplet size determination, stability, in vitro release, in vivo bioavailability and tissue distribution experiments. Results shown that the SMEDDS of CA has a high self-emulsifying rate (>98%) in the dissolution media, and its microemulsion exhibits small droplet size (16...
January 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28088792/impact-of-nudt15-polymorphisms-on-thiopurines-induced-myelotoxicity-and-thiopurines-tolerance-dose
#10
Dandan Yin, Xuyang Xia, Junlong Zhang, Shouyue Zhang, Fei Liao, Ge Zhang, Yan Zhang, Qianqian Hou, Xue Yang, Hong Wang, Zhigui Ma, Heyao Wang, Yiping Zhu, Wei Zhang, Yuelan Wang, Bo Liu, Lanlan Wang, Heng Xu, Yang Shu
Thiopurines are widely used as anticancer and immunosuppressive agents. However, life-threatening myelotoxicity has been noticed and largely explained by genetic variations, including NUDT15 polymorphisms (e.g., rs116855232). In this study, we conduct a meta-analysis to investigate the impact of rs116855232 on thiopurines-induced myelotoxicity susceptibility (1752 patients from 7 independent cohorts), as well as on thiopurines intolerance dose (2745 patients from 13 cohorts). Variant allele of rs116855232 contributes 7...
January 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28088691/stability-effect-of-cholesterol-poly-acrylic-acid-in-a-stimuli-responsive-polymer-liposome-complex-obtained-from-soybean-lecithin-for-controlled-drug-delivery
#11
M G Simões, P Alves, Manuela Carvalheiro, P N Simões
The development of polymer-liposome complexes (PLCs), in particular for biomedical applications, has grown significantly in the last decades. The importance of these studies comes from the emerging need in finding intelligent controlled release systems, more predictable, effective and selective, for applications in several areas, such as treatment and/or diagnosis of cancer, neurological, dermatological, ophthalmic and orthopedic diseases, gene therapy, cosmetic treatments, and food engineering. This work reports the development and characterization of a pH sensitive system for controlled release based on PLCs...
January 4, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28088456/development-of-a-predictive-model-for-the-long-term-stability-assessment-of-drug-in-adhesive-transdermal-films-using-polar-pressure-sensitive-adhesives-as-carrier-matrix
#12
Clémence Chenevas-Paule, Hans-Michael Wolff, Mark Ashton, Martin Schubert, Kalliopi Dodou
Drug crystallization in transdermal drug delivery systems (TDDS) is a critical quality defect. The impact of drug load and hydration on the physical stability of polar (acrylic) drug-in-adhesive (DIA) films was investigated with the objective to identify predictive formulation parameters with respect to drug solubility and long-term stability. Medicated acrylic films were prepared over a range of drug concentrations below and above saturation solubility; and were characterized by FTIR, differential scanning calorimetry (DSC), polarized microscopy and Dynamic Vapor Sorption (DVS) analysis...
January 11, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28088282/conjugation-site-analysis-of-antibody-drug-conjugates-adcs-by-signature-ion-fingerprinting-and-normalized-area-quantitation-approach-using-nano-liquid-chromatography-coupled-to-high-resolution-mass-spectrometry
#13
Hua Sang, Gaoyuan Lu, Yazhong Liu, Qiyue Hu, Weifeng Xing, Dongbing Cui, Fang Zhou, Jingwei Zhang, Haiping Hao, Guangji Wang, Hui Ye
Trastuzumab-MCC-DM1 (T-DM1) is an antibody-drug conjugate (ADC) that consists of a monoclonal antibody (mAb) trastuzumab non-cleavably linked to a cytotoxic drug DM1. During production, the DM1 agents were conjugated to the lysine residues of the mAb in a non-specific manner, yielding a heterogeneous mixture of ADC molecules that differ with respect to both the number and the conjugation sites of DM1 per mAb molecule. Since drug conjugation sites of ADC can significantly impact properties such as stability and pharmacokinetic behaviors, a rapid and reliable approach for conjugation site analysis of ADCs is highly demanded...
February 22, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28088099/protein-templated-synthesis-of-metal-based-nanomaterials
#14
REVIEW
Arnout Rd Voet, Jeremy Rh Tame
There is currently intense interest in using protein scaffolds to prepare uniform nanometre-sized clusters of metals or other inorganic material for use as sensors, imaging agents, drugs, magnetic materials or catalysts. Non-templated chemical synthesis of such clusters often results in a product of variable size and quality, but protein molecules have proved adept at nucleating and stabilizing precise nanoclusters of various kinds. Although much research has focused on natural proteins, such as the iron-storage protein ferritin, recent developments in protein design have allowed entirely novel, symmetrical proteins to be used as templates for the first time...
January 11, 2017: Current Opinion in Biotechnology
https://www.readbyqxmd.com/read/28088003/the-effect-of-the-antioxidant-on-the-properties-of-thiolated-poly-aspartic-acid-polymers-in-aqueous-ocular-formulations
#15
Mária Budai-Szűcs, Gabriella Horvát, Benjámin Gyarmati, Barnabás Áron Szilágyi, András Szilágyi, Szilvia Berkó, Rita Ambrus, Piroska Szabó-Révész, Giuseppina Sandri, Maria Cristina Bonferoni, Carla Caramella, Erzsébet Csányi
Thiolated polymers are a promising new group of excipients, but their stability against atmospheric oxidation has not been investigated in detail, and only a few efforts have been made to improve their stability. The oxidation of the thiol groups in solutions of thiolated polymers may result in a decrease of mucoadhesion and unpredictable in situ gelation. The aims of our work were to study the stability of aqueous solutions of thiolated polymers and the effects of stabilizing agents. We investigated thiolated poly(aspartic acid) polymers stabilized with dithiothreitol, glutathione or acetylcysteine...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087449/highly-biocompatible-chitosan-with-super-paramagnetic-calcium-ferrite-cafe2o4-nanoparticle-for-the-release-of-ampicillin
#16
Ram Bilas, K Sriram, P Uma Maheswari, K M Meera Sheriffa Begum
The CaFe2O4 nanoparticles (CFNP) were synthesized using the solution combustion method. The CFNP-chitosan-ampicillin was prepared by the ionic gelation method using tripolyphosphate (TPP). The CFNP, chitosan-CFNP, chitosan-CFNP-ampicillin materials were characterized by XRD, FT-IR and TGA analysis in order to evaluate the particle nature and size, the presence of functional groups and their thermal stability. The FESEM and EDAX analysis were performed to understand the surface morphology of the materials and the presence of CFNP in the material, respectively...
January 10, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28087407/polymeric-micelles-for-ocular-drug-delivery-from-structural-frameworks-to-recent-preclinical-studies
#17
REVIEW
Abhirup Mandal, Rohit Bisht, Ilva D Rupenthal, Ashim K Mitra
Effective intraocular drug delivery poses a major challenge due to the presence of various elimination mechanisms and physiological barriers that result in low ocular bioavailability after topical application. Over the past decades, polymeric micelles have emerged as one of the most promising drug delivery platforms for the management of ocular diseases affecting the anterior (dry eye syndrome) and posterior (age-related macular degeneration, diabetic retinopathy and glaucoma) segments of the eye. Promising preclinical efficacy results from both in-vitro and in-vivo animal studies have led to their steady progression through clinical trials...
January 10, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28087380/polymeric-mixed-micelles-as-nanomedicines-achievements-and-perspectives
#18
REVIEW
Maximiliano Cagel, Fiorella C Tesan, Ezequiel Bernabeu, Maria J Salgueiro, Marcela B Zubillaga, Marcela A Moretton, Diego A Chiappetta
During the past few decades, polymeric micelles have raised special attention as novel nano-sized drug delivery systems for optimizing the treatment and diagnosis of numerous diseases. These nanocarriers exhibit several in vitro and in vivo advantages as well as increased stability and solubility to hydrophobic drugs. An interesting approach for optimizing these properties and overcoming some of their disadvantages is the combination of two or more polymers in order to assemble polymeric mixed micelles. This review article gives an overview on the current state of the art of several mixed micellar formulations as nanocarriers for drugs and imaging probes, evaluating their ongoing status (preclinical or clinical stage), with special emphasis on type of copolymers, physicochemical properties, in vivo progress achieved so far and toxicity profiles...
January 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087354/effect-of-piroxicam-on-lipid-membranes-drug-encapsulation-and-gastric-toxicity-aspects
#19
Natalia Wilkosz, Sami Rissanen, Małgorzata Cyza, Renata Szybka, Maria Nowakowska, Alex Bunker, Tomasz Róg, Mariusz Kepczynski
Uptake of piroxicam, a non-steroidal anti-inflammatory drug, from the intestines after oral intake is limited due to its low solubility and its wide use is associated with several side effects related to the gastrointestinal tract. In this study, all-atom molecular dynamics (MD) simulations and fluorescent spectroscopy were employed to investigate the interaction of piroxicam in neutral, zwitterionic, and cationic forms with lipid bilayers composed of phosphatidylcholine, cholesterol, and PEGylated lipids. Our study was aimed to assess the potential for encapsulation of piroxicam in liposomal carriers and to shed more light on the process of gastrointestinal tract injury by the drug...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28081462/in%C3%A2-vitro-evaluation-of-biodegradable-lignin-based-nanoparticles-for-drug-delivery-and-enhanced-antiproliferation-effect-in-cancer-cells
#20
Patrícia Figueiredo, Kalle Lintinen, Alexandros Kiriazis, Ville Hynninen, Zehua Liu, Tomás Bauleth-Ramos, Antti Rahikkala, Alexandra Correia, Tomáš Kohout, Bruno Sarmento, Jari Yli-Kauhaluoma, Jouni Hirvonen, Olli Ikkala, Mauri A Kostiainen, Hélder A Santos
Currently, nanosystems have been developed and applied as promising vehicles for different biomedical applications. We have developed three lignin nanoparticles (LNPs): pure lignin nanoparticles (pLNPs), iron(III)-complexed lignin nanoparticles (Fe-LNPs), and Fe3O4-infused lignin nanoparticles (Fe3O4-LNPs) with round shape, narrow size distribution, reduced polydispersity and good stability at pH 7.4. The LNPs showed low cytotoxicity in all the tested cell lines and hemolytic rates below 12% after 12 h of incubation...
January 2, 2017: Biomaterials
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