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drug formulation

Jan Steffel, Peter Verhamme, Tatjana S Potpara, Pierre Albaladejo, Matthias Antz, Lien Desteghe, Karl Georg Haeusler, Jonas Oldgren, Holger Reinecke, Vanessa Roldan-Schilling, Nigel Rowell, Peter Sinnaeve, Ronan Collins, A John Camm, Hein Heidbüchel
The current manuscript is the Executive Summary of the second update to the original Practical Guide, published in 2013. Non-vitamin K antagonist oral anticoagulants (NOACs) are an alternative for vitamin K antagonists (VKAs) to prevent stroke in patients with atrial fibrillation (AF), and have emerged as the preferred choice, particularly in patients newly started on anticoagulation. Both physicians and patients are becoming more accustomed to the use of these drugs in clinical practice. However, many unresolved questions on how to optimally use these agents in specific clinical situations remain...
March 19, 2018: Europace: European Pacing, Arrhythmias, and Cardiac Electrophysiology
Jan Steffel, Peter Verhamme, Tatjana S Potpara, Pierre Albaladejo, Matthias Antz, Lien Desteghe, Karl Georg Haeusler, Jonas Oldgren, Holger Reinecke, Vanessa Roldan-Schilling, Nigel Rowell, Peter Sinnaeve, Ronan Collins, A John Camm, Hein Heidbüchel
The current manuscript is the second update of the original Practical Guide, published in 2013 [Heidbuchel et al. European Heart Rhythm Association Practical Guide on the use of new oral anticoagulants in patients with non-valvular atrial fibrillation. Europace 2013;15:625-651; Heidbuchel et al. Updated European Heart Rhythm Association Practical Guide on the use of non-vitamin K antagonist anticoagulants in patients with non-valvular atrial fibrillation. Europace 2015;17:1467-1507]. Non-vitamin K antagonist oral anticoagulants (NOACs) are an alternative for vitamin K antagonists (VKAs) to prevent stroke in patients with atrial fibrillation (AF) and have emerged as the preferred choice, particularly in patients newly started on anticoagulation...
March 17, 2018: European Heart Journal
Aurelia Vasile, Maria Ignat, Mirela Fernanda Zaltariov, Liviu Sacarescu, Iulian Stoleriu, Dan Draganescu, Mihai Dumitras, Lacramioara Ochiuz
The present study reports the first time use of MCM-41 mesoporous silica as highly efficient carrier for bexarotene - an antineoplastic agent specific for cutaneous T-cell lymphoma treatment. Bexarotene is highly toxic and poor-water soluble, having low bioavailability in the conventional pharmaceutical forms. Comparative uptake of bexarotene on amino-functionalized silica host at various functionalization degrees is discussed in details taking into account all structural features, of matrix as well as properties of the drug molecules...
March 2018: Acta Chimica Slovenica
Luisana Di Cristo, Ciaran Manus Maguire, Karen Mc Quillan, Mattia Aleardi, Yuri Volkov, Dania Movia, Adriele Prina-Mello
Nanoparticles (NP)-based inhalation systems for drug delivery can be administered in liquid form, by nebulization or using pressurized metered dose inhalers, and in solid form by means of dry powder inhalers. However, NP delivery to the lungs has many challenges including the formulation instability due to particle-particle interactions and subsequent aggregation, causing poor deposition in the small distal airways and subsequent alveolar macrophages activity, which could lead to inflammation. This work aims at providing an in vitro experimental design for investigating the correlation between the physico-chemical properties of NP, and their biological behavior, when they are used as NP-based inhalation treatments, comparing two different exposure systems...
March 21, 2018: International Journal of Environmental Research and Public Health
Pradipta Ray, Andrew Torck, Lilyana Quigley, Andi Wangzhou, Matthew Neiman, Chandranshu Rao, Tiffany Lam, Ji-Young Kim, Tae Hoon Kim, Michael Q Zhang, Gregory Dussor, Theodore J Price
Molecular neurobiological insight into human nervous tissues is needed to generate next generation therapeutics for neurological disorders like chronic pain. We obtained human Dorsal Root Ganglia (DRG) samples from organ donors and performed RNA-sequencing (RNA-seq) to study the human DRG (hDRG) transcriptional landscape, systematically comparing it with publicly available data from a variety of human and orthologous mouse tissues, including mouse DRG (mDRG). We characterized the hDRG transcriptional profile in terms of tissue-restricted gene co-expression patterns and putative transcriptional regulators, and formulated an information-theoretic framework to quantify DRG enrichment...
March 20, 2018: Pain
Janicy Arantes Carvalho, Alexandro Silva Abreu, Vitória Tonini Porto Ferreira, Erika Peterson Gonçalves, Antonio Claudio Tedesco, Juliana Guerra Pinto, Juliana Ferreira-Strixino, Milton Beltrame Junior, Andreza Ribeiro Simioni
Gelatin nanoparticles have recently been receiving considerable attention because they offer a good option as release systems due to their low cost, biocompatibility, biodegradability and its application in several types of formulations. This study aim was to evaluate the potential application of gelatin nanoparticles entrapping a photosensitizer in Photodynamic Therapy. Gelatin nanoparticles were studied by steady-state techniques and the biological activity evaluated by in vitro MTT assay. The particles were spherical in shape exhibiting a 273 nm diameter with a low tendency to aggregate...
March 21, 2018: Journal of Biomaterials Science. Polymer Edition
Bayan Alemrayat, Abdelbary Elhissi, Husam M Younes
Letrozole (LTZ), an aromatase inhibitor used for the treatment of hormonally-positive breast cancer in postmenopausal women, has poor water solubility, rapid metabolism and a range of side effects. In this study, polymer-based nanoparticles (NPs) incorporating the drug have been designed and characterized, aimed to control the release, potentially maximize the therapeutic efficiency and minimize the side effects of the drug. LTZ was incorporated into Poly (D, L-Lactide) (PDLLA) NPs by employing the emulsion-solvent evaporation technique using a range of drug concentrations...
March 21, 2018: Pharmaceutical Development and Technology
Mahtab Alam, Abul Kalam Najmi, Iqbal Ahmad, Farhan Jalees Ahmad, Md Jawaid Akhtar, Syed Sarim Imam, Mohd Akhtar
The study performed molecular docking, formulated, characterized thymoquinone (TQ) loaded solid lipid nano particles (TQSLN) and exhibited comparative antidepressant activity. TQ loaded nano lipid formulations were prepared by solvent injection methods and characterize for different in-vitro parameters. The optimized formulation was evaluated for depression using unpredictable chronic mild stress (UCMS) model for a period of six weeks. TQSLN was assessed in modified forced swim test (MFST), tail suspension test (TST), locomotor activity followed by biochemical parameters such as monoaminesand brain derived neurotrophic factor (BDNF)...
March 21, 2018: Artificial Cells, Nanomedicine, and Biotechnology
Kurt Wood, Myron R Szewczuk, Dérick Rousseau, Ronald J Neufeld
Pickering emulsions are colloidal dispersions stabilized by particles that either migrate to, or are formed at, the oil-water interface during emulsification. Here, we fabricated and characterized Pickering water-in-oil emulsions where molten glycerol monostearate crystallized at the surface of micron-sized water droplets and formed protective solid shells. We tested this emulsion as a reservoir delivery platform for the sustained release of low molecular weight hydrophilic molecules including sodium chloride (NaCl) and sodium citrate as model compounds, and the therapeutic oseltamivir phosphate (OP), the delivery of which was the ultimate goal of this research...
February 27, 2018: Oncotarget
Chien-Liang Fang, Yiwei Wang, Kevin H-Y Tsai, Hsin-I Chang
The dermis of human skin contains large numbers of fibroblasts that are responsible for the production of the extracellular matrix (ECM) that supporting skin integrity, elasticity and wound healing. Previously, an in vivo study demonstrated that dermal fibroblasts siting in the lower dermis are capable to convert into skin adipose layer and hence fibroblast lipogenesis may vary the structure and elasticity of dermis. In the present study, Hs68 human dermal fibroblasts were utilized as an in vitro model to study the lipogenesis via using adipogenic differentiation medium (ADM)...
2018: Frontiers in Pharmacology
Eva Ceskova, Petr Silhan
In spite of tremendous development in central nervous system research, current treatment is suboptimal, especially in severe mental disorders. In medicine, there are two main methods of improving the health care provided: seeking new treatment procedures and perfecting (optimizing) the existing ones. Optimization of treatment includes not only practical tools such as therapeutic drug monitoring but also implementation of general trends in the clinical practice. New pharmacological options include new more sophisticated forms of monoaminergic drugs, old drugs rediscovered on the base of a better understanding of pathophysiology of mental illnesses, and drugs aimed at new treatment targets...
2018: Neuropsychiatric Disease and Treatment
Yue Zhang, Liying Zhang, Qi Zhang, Xitong Zhang, Tong Zhang, Bing Wang
Background: Brucea javanica oil (BJO), a traditional Chinese herbal medicine, has a variety of pharmacological activities and several BJO-related patent drugs have been widely used in China. Purpose: The objective of this study was to evaluate the gastric therapeutic effects of self-made BJO and its pharmaceutical potential to formulate novel BJO gastroretentive floating bead by comparing with commercial products. Methods: BJO was extracted from the seeds of B...
2018: Drug Design, Development and Therapy
Basel Arafat, Magdalena Wojsz, Abdullah Isreb, Robert T Forbes, Mohammad Isreb, Waqar Ahmed, Tawfiq Arafat, Mohamed A Alhnan
Fused deposition modelling (FDM) 3D printing has shown the most immediate potential for on-demand dose personalisation to suit particular patient's needs. However, FDM 3D printing often involves employing a relatively large molecular weight thermoplastic polymer and results in extended release pattern. It is therefore essential to fast-track drug release from the 3D printed objects. This work employed an innovative design approach of tablets with unique built-in gaps (Gaplets) with the aim of accelerating drug release...
March 17, 2018: European Journal of Pharmaceutical Sciences
Emilie Bahne, Andreas Brønden, Tina Vilsbøll, Filip Krag Knop
Metformin is an oral anti-hyperglycaemic drug used as first-line treatment of Type 2 diabetes. It is more effective when administered orally than when administered intravenously, and metformin formulations, which prolong the time residing in the gut are the most potent. This indicates that the intestine plays an essential role in metformin's mode of action. Metformin also increases plasma concentrations of the glucose-lowering gut incretin hormone glucagon-like peptide-1 (GLP-1). This metformin-induced GLP-1 increment may constitute an important link between the gut and the glucose-lowering effect of metformin...
March 19, 2018: Ugeskrift for Laeger
Aftab Ahmad, Mohammed F Abuzinadah, Huda M Alkreathy, Babajan Banaganapalli, Mohd Mujeeb
BACKGROUND: Ursolic acid (UA) is a promising molecule with anti-inflammatory, analgesic and potential anti-arthritic activity. METHODS: This study was undertaken to make formulation and evaluation of Ocimum sanctum L. leaf extract (OLE) loaded nano-structured lipid carriers (OLE-NLCs) for improved transdermal delivery of UA. Different surfactants, solid lipids and liquid lipids were used for the preparation of NLCs. The NLCs were developed using emulsion solvent diffusion and evaporation method...
2018: PloS One
Peddi Maharshi, Sachin Kumar Singh, Monica Gulati, Ankit Kumar Yadav, Varun Garg, Bimlesh Kumari, K Gowthamarajan
A major challenge in targeting orally administered drugs to colon is their passage through the long gastrointestinal path comprising highly variant conditions in terms of pH, viscosity, gut motility and microbial flora. Approaches of pH controlled release and microbially triggered release have proved to be successful in achieving colon targeting only to a partial extent. In an attempt to improve targeting, both these approaches have been combined together with the approach of liquisolid technology which, hitherto, remains unexplored for colon targeting...
March 19, 2018: Current Drug Delivery
Samane Bayrami, Zahra Esmaili, SeyedAhmad SeyedAlinaghi, Saeed Reza Jamali Moghadam, Sepide Bayrami, Hamid AkbariJavar, Morteza Rafiee Tehrani, Farid Abedin Dorkoosh
The purpose of this research was the fabrication, statistical optimization and in vitro characterization of insulin loaded poly (hydroxybutyrate-co-hydroxyvalerate) (PHBV) nanoparticles (INS-PHBV-NPs). Nanoparticles were successfully developed by double emulsification solvent evaporation method. The NPs were characterized for particle size, entrapment efficiency (EE %), polydispersity index (PDI). The NPs also were characterized by SEM, FT-IR, XRD, DSC and CD. The optimum conditions were found to be 1.6% polyvinyl alcohol (PVA), 0...
March 20, 2018: Pharmaceutical Development and Technology
Diana E Aziz, Aly A Abdelbary, Abdelhalim I Elassasy
Diacerein (DCN) is a hydrophobic osteoarthritis (OA) drug with short half-life and low oral bioavailability. Furthermore, DCN oral administration is associated with diarrhea which represents obstacle against its oral use. Hence, this article aimed at developing elastosomes (edge activator (EA)-based vesicular nanocarriers) as a novel transdermal system for delivering DCN efficiently and avoiding its oral problems. For achieving this goal, elastosomes were prepared according to 41 .21 full factorial design using different EAs in varying amounts...
November 2018: Drug Delivery
Margaret R Caplan, Eric S Daar, Katya C Corado
Treatment options for patients with HIV-1 infection have grown over the past two decades to include multiple fixed-dose combination pharmacotherapies that have greatly simplified administration of antiretroviral therapy (ART) for both patients and providers. Effective virologic control can often be achieved with once-daily use of a single-tablet regimen. Over the past three years, ART drug development has focused on the next generation of fixed-dose combinations for initial and maintenance therapy with improved efficacy, safety and tolerability...
March 20, 2018: Expert Opinion on Pharmacotherapy
Kavitha Ranganathan, Eric Simon, Jeremy Lynn, Alicia Snider, Yu Zhang, Noah Nelson, Alexis Donneys, Jose Rodriguez, Lauren Buchman, Dawn Reyna, Elke Lipka, Steven R Buchman
PURPOSE: Amifostine (AMF), a radioprotectant, is FDA-approved for intravenous administration in cancer patients receiving radiation therapy (XRT). Unfortunately, it remains clinically underutilized due to adverse side effects. The purpose of this study is to define the pharmacokinetic profile of an oral AMF formulation potentially capable of reducing side effects and increasing clinical feasibility. METHODS: Calvarial osteoblasts were radiated under three conditions: no drug, AMF, and WR-1065 (active metabolite)...
March 19, 2018: Pharmaceutical Research
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