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https://www.readbyqxmd.com/read/29156348/development-of-photoprotective-antiphototoxic-and-antiphotogenotoxic-formulations-of-ocular-drugs-with-fluoroquinolones
#1
Anna Zgadzaj, Joanna Kornacka, Anita Jastrzębska, Andrzej Parzonko, Sylwester Sommer, Grzegorz Nałęcz-Jawecki
The development of innovative solutions in photosafety of photolabile pharmaceutical products may help to reduce the adverse effects of these products, caused by light exposure. Providing new data in this area of study is particularly important in case of drugs applied topically on sensitive organs such as eyes. The main goal of this research is to investigate whether two potential excipients, namely: p-coumaric acid and benzophenone-4, affect the photodegradation, phototoxicity and photogenotoxicity of water solutions of four fluoroquinolones: ciprofloxacin, lomefloxacin, fleroxacin and clinafloxacin...
November 9, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29155732/fabrication-and-characterization-of-griffithsin-modified-fiber-scaffolds-for-prevention-of-sexually-transmitted-infections
#2
Hung R Vuong, Kevin M Tyo, Jill M Steinbach-Rankins
Electrospun fibers (EFs) have been widely used in a variety of therapeutic applications; however, they have only recently been applied as a technology to prevent and treat sexually transmitted infections (STIs). Moreover, many EF technologies focus on encapsulating the active agent, relative to utilizing the surface to impart biofunctionality. Here we describe a method to fabricate and surface-modify poly(lactic-co-glycolic) acid (PLGA) electrospun fibers, with the potent antiviral lectin Griffithsin (GRFT)...
October 31, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/29155283/comparative-analysis-of-media-effects-on-human-induced-pluripotent-stem-cell-derived-cardiomyocytes-in-proarrhythmia-risk-assessment
#3
Derek Schocken, Jayna Stohlman, Jose Vicente, Dulciana Chan, Dakshesh Patel, Murali Krishna Matta, Vikram Patel, Mathew Brock, Daniel Millard, James Ross, David G Strauss, Ksenia Blinova
INTRODUCTION: Cardiotoxicity assessment using human induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs) forms a key component of the Comprehensive in Vitro Proarrhythmia Assay (CiPA). A potentially impactful factor on iPSC-CM testing is the presence of serum in the experimental media. Generally, serum-free media is used to most accurately reproduce "free" drug concentration. However, caution is needed; drug solubility and cardiomyocyte electrophysiology could be affected by media formulation, potentially impacting interpretation of drug-induced effects...
November 16, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/29155074/photodynamic-diagnosis-of-parathyroid-glands-with-nano-stealth-aminolevulinic-acid-liposomes
#4
Shaimaa Elbassiouny, Maha Fadel, Tarek Elwakeel, Mahmoud Saber
AIM OF THE STUDY: Exploring whether the formulation of ALA in nano-stealth liposomes would inflict its photodiagnostic effectiveness. The present study represents ALA in nano-stealth liposomes as well as in conventional nanoliposomes in order to be used for photodiagnosis of parathyroid glands intraoperatively. MATERIALS AND METHODS: Preparation of ALA nanovesicles and characterization for the drug encapsulation%, vesicle size, Zeta potential, in vitro drug release profile and stability...
November 15, 2017: Photodiagnosis and Photodynamic Therapy
https://www.readbyqxmd.com/read/29155053/alpha-tocopherol-loaded-chitosan-oleate-nanoemulsions-for-wound-healing-evaluation-on-cell-lines-and-ex-vivo-human-biopsies-and-stabilization-in-spray-dried-trojan-microparticles
#5
M C Bonferoni, F Riva, A Invernizzi, E Dellera, G Sandri, S Rossi, G Marrubini, G Bruni, B Vigani, C Caramella, F Ferrari
An amphiphilic chitosan salt, chitosan oleate (CS-OA), was previously proposed for the physical stabilization of lemongrass antimicrobial nanoemulsions (NE) through a mild spontaneous emulsification process. As both chitosan and oleic acid are described in the literature for their positive effects in wound healing, in the present study CS-OA has been proposed to encapsulate alpha tocopherol (αTph) in NEs aimed to skin wounds. A NE formulation was developed showing about 220 nm dimensions, 36% drug loading, and αTph concentration up to 1 mg/ml...
November 15, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29154900/alternative-manufacturing-concepts-for-solid-oral-dosage-forms-from-drug-nanosuspensions-using-fluid-dispensing-and-forced-drying-technology
#6
Bastian Bonhoeffer, Arno Kwade, Michael Juhnke
Flexible manufacturing technologies for solid oral dosage forms with a continuous adjustability of the manufactured dose strength, are of interest for applications in personalized medicine. This study explored the feasibility of using micro-valve technology for the manufacturing of different solid oral dosage form concepts. Hard gelatin capsules filled with excipients, placebo tablets and polymer films, placed in hard gelatin capsules after drying, were considered as substrates. For each concept a basic understanding of relevant formulation parameters and their impact on dissolution behavior has been established...
November 15, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29154881/influence-of-polymer-ratio-and-surfactants-on-controlled-drug-release-from-cellulosic-microsponges
#7
Yasser Shahzad, Sidra Saeed, Muhammad Usman Ghori, Tariq Mahmood, Abid Mehmood Yousaf, Muhammad Jamshaid, Rizwan Sheikh, Syed A A Rizvi
Microsponge refers to a highly cross-linked particle system with a capacity to adsorb (like a dry sponge) pharmaceutical materials. There are various methods available to prepare microsponge formulations, in this study we used quasi emulsion-solvent diffusion method with a combination of hydrophobic (ethyl cellulose) and hydrophilic polymers (hydroxypropyl methylcellulose) mediated via Tween 80 and polyvinyl alcohol. Various ratios and amounts of the polymers and surfactants were used to prepare microsponge formulations using ketoprofen as a model drug and extensively characterised...
November 14, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29154834/development-and-characterization-of-docetaxel-loaded-lecithin-stabilized-micellar-drug-delivery-system-lsbmdds-for-improving-the-therapeutic-efficacy-and-reducing-systemic-toxicity
#8
Chia-Yu Su, Jun-Jen Liu, Yuan-Soon Ho, Yi-You Huang, Vincent Hung-Shu Chang, Der-Zen Liu, Ling-Chun Chen, Hsiu-O Ho, Ming-Thau Sheu
In the present study, we attempted to develop a lecithin-stabilized micellar drug delivery system (LsbMDDs) for loading docetaxel (DTX) to enhance its therapeutic efficacy and minimize systemic toxicity. A novel DTX-loaded LsbMDDs was optimally prepared by a thin-film hydration method and then hydrated with a lecithin nanosuspension while being subjected to ultrasonication. Physical characteristics of the optimized DTX-loaded LsbMDDs formulations were examined and found to have a mean size of <200 nm, an encapsulation efficiency of >90%, and drug loading of >6% with stability at room temperature and at 4° C being longer than 2 and 7 days, respectively...
November 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29154213/liposomally-formulated-phospholipid-conjugated-novel-near-infrared-fluorescence-probe-for-particle-size-effect-on-cellular-uptake-and-biodistribution-in-vivo
#9
Jing Xing, Dong Liu, Gaoxin Zhou, Yuan Li, Peng Wang, Ke Hu, Ning Gu, Min Ji
Lipid based nanoparticles (LBNs) with excellent biocompatibility and versatility have received much attention from the drug delivery community recently. A detailed understanding of in vitro and vivo fate of LBNs is important for developing different types of LBNs with improved selectivity and low cytotoxicity. We developed a novel near-infrared (NIR) probe with high fluorescence, designated as DSPE-ir623 (iDSPE). Then, we prepared iDSPE-embeded liposomes (iLPs) with two different hydrodynamic sizes (∼100nm and ∼400nm) to evaluate the effect of particle size on cellular uptake and biodistribution of nanoliposomes in vivo...
November 16, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29154189/novel-theranostic-zinc-phthalocyanine-phospholipid-complex-self-assembled-nanoparticles-for-imaging-guided-targeted-photodynamic-treatment-with-controllable-ros-production-and-shape-assisted-enhanced-cellular-uptake
#10
Jinyuan Ma, Yang Li, Guihua Liu, Ai Li, Yilin Chen, Xinyi Zhou, Dengyue Chen, Zhenqing Hou, Xuan Zhu
The novel drug delivery system based on self-assembly of zinc phthalocyanine-soybean phosphatidylcholine (ZnPc-SPC) complex was developed by a co-solvent method followed by a nanoprecipitaion technique. DSPE-PEG-methotrexate (DSPE-PEG-MTX) was introduced on the surface of ZnPc-SPC self-assembled nanoparticles (ZS) to endow them with folate receptor-targeting property. NMR, XRD, FTIR, and UV-vis-NIR analysis demonstrated the weak molecular interaction between ZnPc and SPC. The ZS functionalized with DSPE-PEG-MTX (ZSPM) was successfully constructed with an average particle size of ∼170nm, a narrow size distribution, and could remain physiologically stable for at least 7days...
October 24, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29154026/inhibitors-of-metallo-%C3%AE-lactamases
#11
REVIEW
Caitlyn M Rotondo, Gerard D Wright
The β-lactams are the most successful class of antibiotic drugs but they are vulnerable to inactivation by a growing cadre of β-lactamases that now number more than a thousand variants. β-Lactamases operate by one of two general chemical mechanisms either catalyzing β-lactam ring hydrolysis via a covalent enzyme intermediate through the aegis of an active site serine residue or through a noncovalent Zn-dependent mechanism. The Ser-β-lactamases are currently dominant in the clinic and consequently, there has been great effort to identify inhibitors and to co-formulate these with β-lactam antibiotics...
November 15, 2017: Current Opinion in Microbiology
https://www.readbyqxmd.com/read/29153926/pharmacokinetics-of-risperidone-in-different-application-forms-comparing-long-acting-injectable-and-oral-formulations
#12
Georgios Schoretsanitis, Jose de Leon, Ekkehard Haen, Benedikt Stegmann, Christoph Hiemke, Gerhard Gründer, Michael Paulzen
We aimed to explore the differences in the pharmacokinetics of risperidone between oral and long-acting injectable (LAI) formulations using a large database of therapeutic drug monitoring (TDM). Plasma concentrations of risperidone (RIS), its active metabolite (9-OH-RIS) and the active moiety (AM) (RIS+9-OH-RIS), their concentration-to-dose (C/D) ratios and ratio of RIS/9-OH-RIS (an index of CYP2D6 metabolic activity) were used to compare patients receiving risperidone orally (n = 851) and those treated with LAI RIS (n = 63)...
November 16, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29153580/effectiveness-and-safety-of-oro-dispersible-sildenafil-in-a-new-film-formulation-for-the-treatment-of-erectile-dysfunction-comparison-between-sildenafil-100-mg-film-coated-tablet-and-75-mg-oro-dispersible-film
#13
Andrea Cocci, Marco Capece, Gianmartin Cito, Giorgio Ivan Russo, Marco Falcone, Massimiliano Timpano, Michele Rizzo, Pier Andrea Della Camera, Simone Morselli, Riccardo Campi, Francesco Sessa, Giovanni Cacciamani, Andrea Minervini, Mauro Gacci, Vincenzo Mirone, Girolamo Morelli, Nicola Mondaini, Gaia Polloni, Sergio Serni, Alessandro Natali
BACKGROUND: A new oro-dispersible film (ODF) formulation of sildenafil has been developed for the treatment of erectile dysfunction (ED) to overcome the drawbacks that some patients experience when taking the conventional film-coated tablet (FCT). AIM: To assess the effectiveness and safety of sildenafil ODF formulation in patients with ED who were using the conventional FCT. METHODS: From May 2017 through July 2017, 139 patients with ED were enrolled...
November 16, 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29152677/adhd-and-anxiety-clinical-significance-and-treatment-implications
#14
REVIEW
Frederick W Reimherr, Barrie K Marchant, Thomas E Gift, Tammy A Steans
In comparison to the DSM formulation of ADHD, we have proposed that ADHD in adults should be divided into Inattentive and Emotional Dysregulation Presentations. Under both systems, there is potential overlap with generalized anxiety disorder (GAD). We compared data from four distinct populations: ADHD clinical trials, GAD clinical trials, an ADHD clinic, and a forensic clinic. Approximately 25% of patients in each population had comorbid ADHD and anxiety. Comorbid subjects reported more childhood ADHD symptoms and higher scores on ADHD scales and were more likely to fit criteria for ADHD Emotional Dysregulation Presentation or DSM-IV combined type...
November 20, 2017: Current Psychiatry Reports
https://www.readbyqxmd.com/read/29152321/impact-of-the-number-of-repeated-inhalations-and-patient-characteristics-on-the-residual-amount-of-inhaled-laninamivir-octanoate-hydrate-dry-powder-in-pediatric-patients-with-influenza
#15
Toshiki Murasaka, Kenji Ikemura, Tomoyuki Enokiya, Yuichi Muraki, Mayumi Ikemura, Koji Terada, Takuya Iwamoto, Masahiro Okuda
Background: A dry powder inhaled formulation is used for the anti-influenza drug laninamivir octanoate hydrate (laninamivir). Although two successive inhalations (puffs) are recommended to minimize residual amounts of active ingredients, previous reports suggest that pediatric patients with low peak inspiratory flow are unable to inhale the active ingredient adequately. In the present study, we prospectively investigated the appropriate number of repeated inhalations of laninamivir dry powder and factors influencing the residual amount of ingredients in pediatric patients with influenza...
2017: Journal of Pharmaceutical Health Care and Sciences
https://www.readbyqxmd.com/read/29152080/vincristine-liposomes-with-smaller-particle-size-have-stronger-diffusion-ability-in-tumor-and-improve-tumor-accumulation-of-vincristine-significantly
#16
Siyu Ma, Mingyuan Li, Nan Liu, Ying Li, Zhiping Li, Yang Yang, Fanglin Yu, Xiaoqin Hu, Cheng Liu, Xingguo Mei
The passive targeting is the premise of active targeting that could make nanocarrier detained in tumor tissue. The particle size is the most important factor that influences the diffusion and distribution of nanoparticle both in vivo and in vitro. In order to investigate the relationship between particle size and diffusion ability, two kinds of liposome loaded with Vincristine (VCR-Lip) were prepared. The diffusion behavior of VCR-Lip with different particle size and free VCR was compared through diffusion stability study...
October 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/29151132/safety-of-intrathecal-route-focus-to-methylprednisolone-acetate-depo-medrol-use
#17
REVIEW
Joël Schlatter, David Nguyen, Michèle Zamy, Sofiane Kabiche, Jean-Eudes Fontan, Salvatore Cisternino
PURPOSE: Complications of the intrathecal route may cause potential toxicity related to the medical device and properties of the administered drug and/or excipient. A description of clinical and histological effects of polyethylene glycol and miripirium after Depo-Medrol injection, and the adverse reactions of particulate methylprednisolone acetate was conducted. The safety of the intrathecal route with excipients, label and off-label drugs is discussed. METHODS: A bibliographic search in Medline, Google, and Cochrane database from 1940 to June 2016 was performed...
November 18, 2017: European Spine Journal
https://www.readbyqxmd.com/read/29150845/effect-of-sorbitol-on-the-pharmacokinetic-profile-of-lamivudine-oral-solution-in-adults-an-open-label-randomized-study
#18
Kimberly Adkison, Allen Wolstenholme, Yu Lou, Zhiping Zhang, Amy Eld, Teodora Perger, Harald Vangerow, Katy Hayward, Mark Shaefer, Cynthia McCoig
In children aged ≤4 years, the relative bioavailability of lamivudine oral solution was 37% lower than that of a tablet formulation. An open-label, 4-way crossover study was conducted in healthy adults to evaluate the effect of sorbitol, a common liquid excipient, on the pharmacokinetics of lamivudine oral solution (ClinicalTrials.gov identifier, NCT02634073). Sixteen subjects were randomized to 1 of 4 sequences consisting of 4 doses of lamivudine 300 mg (10 mg/mL) alone or with sorbitol 3.2, 10.2, or 13...
November 18, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29150770/population-in-vitro-in-vivo-pharmacokinetic-model-of-first-pass-metabolism-itraconazole-and-hydroxy-itraconazole
#19
Ahmad Y Abuhelwa, Stuart Mudge, Richard N Upton, David J R Foster
The aim of this study was to develop a population in vitro-in vivo pharmacokinetic model that simultaneously describe the absorption and accumulation kinetics of itraconazole (ICZ) and hydroxy-itraconazole (HICZ) in healthy subjects. The model integrated meta-models of gastrointestinal pH and gastrointestinal transit time and in vitro dissolution models of ICZ with the absorption and disposition kinetics of ICZ and HICZ. Mean concentration intravenous data, and single- and multi-dose oral data were used for model development...
November 17, 2017: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/29150282/artesunate-quercetin-luteolin-dual-drug-nanofacilitated-synergistic-treatment-for-malaria-a-plausible-approach-to-overcome-artemisinin-combination-therapy-resistance
#20
Nethravathi Puttappa, Raman Suresh Kumar, Karthik Yamjala
Malaria is one of the major global health challenge with 300 million new cases annually. The best regimen for treating Plasmodium falciparum induced malaria is based on artemisinin and its derivatives which were prescribed as artemisinin combination therapy (ACT). These are highly effective drugs resulting in rapid clearance of parasites even in severe P. falciparum induced malaria patients. However, from the past few years parasites resistant to ACT's have begun to emerge in various parts of the world such as Cambodia and Greater Mekong Subregion...
November 2017: Medical Hypotheses
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