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Drug release

Yuan-Bo Wu, Li Zhang, Wen-Ting Li, Yi Yang, Jiang-Ming Zhao
BACKGROUND: Artesunate (ART) is an antimalarial drug with potential anti-inflammatory effect. This study aimed to explore the potential protective role of ART in hepatic encephalopathy (HE), involving its function against ammonia toxicity. METHODS: HE rats were induced by the administration of thioacetamide (TAA, 300mg/kg/day). Spatial learning ability was tested in both Morris water and eight-arm radial maze. Rat cerebellar granule neurons (CGNs) were prepared for ammonia treatment in vitro, in line with SH-SY5Y and C6 cells...
October 17, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Sandrine Alibert, Joannah N'Gompazza Diarra, Jessica Hernandez, Aurélien Stutzmann, Marwa Fouad, Gérard Boyer, Jean-Marie Pagès
Worrying levels of bacterial resistance have been reported worldwide involving the failure of many available antibiotic treatments. Multidrug resistance (MDR) in Gram-negative bacteria is often ascribed to the presence of multiple and different resistance mechanisms in the same strain. RND efflux pumps play a major role and are an attractive target to discover new antibacterial drugs. Areas covered: This review discusses the prevalence of efflux pumps, their overexpression in clinical scenarios, their polyselectivity, their effect on the intracellular concentrations of various antibiotics associated with the alteration of the membrane permeability and their involvement in pathogenicity are discussed...
October 20, 2016: Expert Opinion on Drug Metabolism & Toxicology
Matthew Thomas Sims, Zachary Carter Sanchez, James Murphy Herrington, James Barrett Hensel, Nolan Michael Henning, Caleb Josiah Scheckel, Matt Vassar
INTRODUCTION: With the intent of improving transparency in clinical research, the International Committee of Medical Journal Editors (ICMJE) established guidelines in 2005 regarding prospective clinical trial registration. This action worked to address bias related to selective outcome reporting in the medical literature. The objective of this study was to assess and characterize the quality of registration of clinical trials appearing in shoulder arthroplasty-related medical journals...
2016: PloS One
O Lidický, M Šírová, T Etrych
In this paper, we describe the synthesis, physicochemical characterization, drug release kinetics and preliminary biological evaluation of several N-(2-hydroxypropyl)methacrylamide (HPMA)-based polymer-retinoid conjugates designed for solid tumor immunotherapy. The conjugates are supposed to inhibit the immunosuppressive activity of myeloid-derived suppressor cells (MDSC) accumulated in the solid tumor microenvironment. All-trans retinoic acid (ATRA) was derivatized to hydrazide (AtrHy) and then attached to the polymer backbone via a spacer that is stable at the normal pH of blood (7...
October 20, 2016: Physiological Research
R Pola, O Janoušková, T Etrych
Cytarabine is one of the most efficient drugs in the treatment of hematological malignancies. In this work, we describe the synthesis and characterization of two different polymer conjugates of cytarabine that were designed for the controlled release of cytarabine within the leukemia cells. Reactive copolymers of N-(2-hydroxypropyl)methacrylamide (HPMA) and 3-(3-methacrylamidopropa-noyl)thiazolidine-2-thione) or 3-(Nmethacryloylglycyl-phenylalanylleucylglycyl)thiazolidine-2-thione were used in the study as reactive polymer precursors for reaction with cytarabine...
October 20, 2016: Physiological Research
J Panek, E Koziolova, P Stepanek, T Etrych, O Janouskova
Nanocarriers bearing anticancer drugs are promising candidates to improve the efficacy of cancer therapy and minimize side effects. The most potent cytostatics used in the treatment of various cancers are anthracyclines, e.g. doxorubicin or pirarubicin. Recently, polymer therapeutics carrying anthracyclines have been intensively studied. The precise characterization of in vitro nanocarrier biological behavior brings a better understanding of the nanocarrier characteristics and enables prediction of the behavior of the nanocarrier during in vivo application...
October 20, 2016: Physiological Research
M Hrubý, S K Filippov, P Štěpánek
Self-organization in a polymer system appears when a balance is achieved between long-range repulsive and short-range attractive forces between the chemically different building blocks. Block copolymers forming supramolecular assemblies in aqueous media represent materials which are extremely useful for the construction of drug delivery systems especially for cancer applications. Such formulations suppress unwanted physicochemical properties of the encapsulated drugs, modify biodistribution of the drugs towards targeted delivery into tissue of interest and allow triggered release of the active cargo...
October 20, 2016: Physiological Research
Pelin Erkoc, Ahmet Cingöz, Tugba Bagci Onder, Seda Kizilel
Overcoming drug resistance is a major challenge for cancer therapy. Tumor necrosis factor α-related apoptosis-inducing ligand (TRAIL) is a potent therapeutic as an activator of apoptosis, particularly in tumor but not in healthy cells. However, its efficacy is limited by the resistance of tumor cell populations to the therapeutic substance. Here, we have addressed this limitation through the development of a controlled release system, matrix-metalloproteinase (MMP)-sensitive and arg-gly-asp-ser (RGDS) peptide functionalized poly (ethylene-glycol) (PEG) particles which are synthesized via visible-light-induced water-in-water emulsion polymerization...
October 20, 2016: Macromolecular Bioscience
Caiyan Zhao, Leihou Shao, Jianqing Lu, Chenying Zhao, Yujie Wei, Junxing Liu, Mingjun Li, Yan Wu
Stimuli-responsive nanocarriers with the ability to respond to tumorous heterogeneity have been extensively developed for drug delivery. However, the premature release during blood circulation and insufficient intracellular drug release are still a significant issue. Herein, three disulfide bonds are introduced into the amphiphilic poly(ethylene glycol)-polycaprolactone copolymer blocks to form triple-sensitive cleavable polymeric nanocarrier (tri-PESC NPs) to improve its sensitivity to narrow glutathione (GSH) concentration...
October 20, 2016: Macromolecular Bioscience
Animesh Pardanani
: Disease overview:Systemic mastocytosis (SM) results from a clonal proliferation of abnormal mast cells (MC) in one or more extra-cutaneous organs. DIAGNOSIS: The major criterion is presence of multifocal clusters of morphologically abnormal MC in the bone marrow. Minor diagnostic criteria include elevated serum tryptase level, abnormal MC expression of CD25 and/or CD2, and presence of KITD816V. Risk stratification: The 2008 World Health Organization (WHO) classification of SM has been shown to be prognostically relevant...
November 2016: American Journal of Hematology
Joaquim Suñer-Carbó, Antonio Boix-Montañés, Lyda Halbaut-Bellowa, Nelvis Velázquez-Carralero, Joanna Zamarbide-Ledesma, Nuria Bozal-de-Febrer, Ana Cristina Calpena-Campmany
Local delivery of imidazolic antifungals is limited by its extreme lipophilicity. Multiple emulsions (ME) are a potential vehicle to enhance the delivery of econazole nitrate (ECN), an antifungal targeted to deep-seated epidermal yeast infections. An 1% ECN hydrophilic ME was compared with a commercial formulation in terms of rheology, droplet size and in vitro antifungal activity against Candida species. Comparative in vitro drug release, human skin permeation and drug retention were investigated using vertical diffusion cells...
October 20, 2016: Mycoses
Dorle Hennig, Diana Imhof
Incorporation of drugs into particles can improve their therapeutic effectiveness. Solubility, half-life time, targeting, and the release of the drug can be modified by the encapsulation into a particle. Histone deacetylase inhibitors have a great potential to be used as therapeutics for many different diseases. In this chapter, we describe the inclusion of the low molar mass HDACi Ex527 into polymer-based particles and liposomes.
2017: Methods in Molecular Biology
Yushu Yin, Georgia Papavasiliou, Olga Y Zaborina, John C Alverdy, Fouad Teymour
The human gastrointestinal tract is the primary site of colonization of multidrug resistant pathogens and the major source of life-threatening complications in critically ill and immunocompromised patients. Eradication measures using antibiotics carry further risk of antibiotic resistance. Furthermore, antibiotic treatment can adversely shift the intestinal microbiome toward domination by resistant pathogens. Therefore, approaches directed to prevent replacement of health promoting microbiota with resistant pathogens should be developed...
October 19, 2016: Annals of Biomedical Engineering
Naader Alizadeh, Ehsan Shamaeli, Masooma Fazili
PURPOSE: The potential of electrochemical/temperature dual stimuli-responsive conducting polymer to be used as general drug delivery systems. It allows on-demand release of incorporated drug is kinetically investigated in real time. METHODS: Online spectroscopic monitoring was used to investigate the electrochemically/thermally controlled release behavior of a model drug (naproxen) from drug-doped polypyrrole (DDPPy) film. Avrami's equation has been used to study the kinetics and further analyzing has been carried out using the Arrhenius and the Eyring equations...
October 19, 2016: Pharmaceutical Research
Koushik Sarkar, Mithun Paul, Parthasarathi Dastidar
Cu(ii) metal-organic-polyhedra (MOP) derived from a tris-pyridyl ligand gave stable single-layered vesicles capable of encapsulating an anti-cancer drug (doxorubicin - DOX) and its pH responsive release. While encapsulation of DOX was further confirmed by MTT assay and cellular imaging, α-chymotrypsin inhibition assay corroborated well with the single crystal structures of the MOP. The MOP derived vesicles reported herein not only represent the rare examples of such hierarchical architectures derived from MOP but also provide the first example of multifunctional organic-inorganic synthetic bio-membranes...
October 20, 2016: Chemical Communications: Chem Comm
Nikolaos Tsamandouras, Tomasz Kostrzewski, Cynthia L Stokes, Linda G Griffith, David J Hughes, Murat Cirit
In this work, we first describe the population variability in hepatic drug metabolism using cryopreserved hepatocytes from 5 different donors cultured in a perfused 3D human liver microphysiological system and then show how the resulting data can be integrated with a modeling and simulation framework to accomplish in vitro-in vivo translation. For each donor, metabolic depletion profiles of 6 compounds (phenacetin, diclofenac, lidocaine, ibuprofen, propranolol and prednisolone) were measured, along with metabolite formation, mRNA levels of 90 metabolism-related genes, and markers of functional viability (LDH release, albumin and urea production)...
October 19, 2016: Journal of Pharmacology and Experimental Therapeutics
Carlos F Cáceres, Annick Borquez, Jeffrey D Klausner, Rachel Baggaley, Chris Beyrer
BACKGROUND: In this article, we present recent evidence from studies focused on the implementation, effectiveness and cost-effectiveness of pre-exposure prophylaxis (PrEP) for HIV infection; discuss PrEP scale-up to date, including the observed levels of access and policy development; and elaborate on key emerging policy and research issues to consider for further scale-up, with a special focus on lower-middle income countries. DISCUSSION: The 2015 WHO Early Release Guidelines for HIV Treatment and Prevention reflect both scientific evidence and new policy perspectives...
2016: Journal of the International AIDS Society
Jingjing Hu, Yihua Chen, Yunqi Li, Zhengjie Zhou, Yiyun Cheng
The development of thermo-degradable hydrogels is of great importance in drug delivery. However, it still remains a huge challenge to prepare thermo-degradable hydrogels with inherent degradation, reproducible, repeated and tunable dosing. Here, we reported a thermo-degradable hydrogel that is rapidly degraded above 44 °C by a facile chemistry. Besides thermo-degradability, the hydrogel also undergoes rapid photolysis with ultraviolet light. By embedding photothermal nanoparticles or upconversion nanoparticles into the gel, it can release the entrapped cargoes such as dyes, enzymes and anticancer drugs in an on-demand and dose-tunable fashion upon near-infrared light exposure...
October 11, 2016: Biomaterials
Guoxin Tan, Shihui Yu, Hao Pan, Jinyu Li, Dandan Liu, Kun Yuan, Xinggang Yang, Weisan Pan
The aim of this study was to develop and characterize a novel colloidal system, namely, timolol maleate chitosan coated liposomes (TM-CHL) to enhance the ocular permeation, precorneal residence time and bioavailability. The resulting TM-CHL was the most promising formulation with a mean particle size of 150.7nm and an EE% of 75.83±1.61%. In vitro release of the TM-CHL showed an extended drug release profile. The TM-CHL exhibited significant mucin adhesion and compared with commercial eye drops, TM-CHL produced a 3...
October 17, 2016: International Journal of Biological Macromolecules
Scott J Hughes, Leanne Barnard, Katayoun Mottaghi, Wolfram Tempel, Tetyana Antoshchenko, Bum Soo Hong, Abdellah Allali-Hassani, David Smil, Masoud Vedadi, Erick Strauss, Hee-Won Park
The potent antistaphylococcal activity of N-substituted pantothenamides (PanAms) has been shown to at least partially be due to the inhibition of Staphylococcus aureus's atypical type II pantothenate kinase (SaPanKII), the first enzyme of coenzyme A biosynthesis. This mechanism of action follows from SaPanKII having a binding mode for PanAms that is distinct from those of other PanKs. To dissect the molecular interactions responsible for PanAm inhibitory activity, we conducted a mini SAR study in tandem with the cocrystallization of SaPanKII with two classic PanAms (N5-Pan and N7-Pan), culminating in the synthesis and characterization of two new PanAms, N-Pip-PanAm and MeO-N5-PanAm...
September 9, 2016: ACS Infectious Diseases
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