Read by QxMD icon Read

Pharmaceutical Research

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
Pei T Mah, Dunja Novakovic, Jukka Saarinen, Stijn Van Landeghem, Leena Peltonen, Timo Laaksonen, Antti Isomäki, Clare J Strachan
PURPOSE: To investigate the effect of compression on the crystallization behavior in amorphous tablets using sum frequency generation (SFG) microscopy imaging and more established analytical methods. METHOD: Tablets containing neat amorphous griseofulvin with/without excipients (silica, hydroxypropyl methylcellulose acetate succinate (HPMCAS), microcrystalline cellulose (MCC) and polyethylene glycol (PEG)) were prepared. They were analyzed upon preparation and storage using attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, scanning electron microscopy (SEM) and SFG microscopy...
October 13, 2016: Pharmaceutical Research
Jeffry Weers, Andy Clark
Current marketed dry powder inhalers utilize the energy from patient inspiration to fluidize and disperse bulk powder agglomerates into respirable particles. Variations in patient inspiratory flow profiles can lead to marked differences in total lung dose (TLD), and ultimately patient outcomes for an inhaled therapeutic. The present review aims to quantitate the flow rate dependence in TLD observed for a number of drug/device combinations using a new metric termed the Q index. With this data in hand, the review explores key attributes in the design of the formulation and device that impact flow rate dependence...
October 13, 2016: Pharmaceutical Research
Lin Zhang, Sandeep Yadav, Barthélemy Demeule, Y John Wang, Olivier Mozziconacci, Christian Schӧneich
PURPOSE: To investigate the mechanisms of polysorbate (PS) degradation with the added objective of differentiating the hydrolysis and oxidation pathways. METHODS: Ultra-performance liquid chromatography mass spectrometry (UPLC-MS) was utilized to characterize all-laurate polysorbate 20 (PS20) and its degradants. (18)O stable isotope labeling was implemented to produce (18)O-labeled degradation products of all-laurate PS20 in H2(18)O, with subsequent UPLC-MS analysis for location of the cleavage site on the fatty acid-containing side chain of PS20...
October 13, 2016: Pharmaceutical Research
Meng-Qing Gong, Cong Wu, Xiao-Yan He, Jing-Yi Zong, Jin-Long Wu, Ren-Xi Zhuo, Si-Xue Cheng
PURPOSE: To overcome multi-drug resistance (MDR) in tumor chemotherapy, a polymer/inorganic hybrid drug delivery platform with tumor targeting property and enhanced cell uptake efficiency was developed. METHOD: To evaluate the applicability of our delivery platform for the delivery of different drug resistance inhibitors, two kinds of dual-drug pairs (doxorubicin/buthionine sulfoximine and doxorubicin/tariquidar, respectively) were loaded in heparin-biotin/heparin/protamine sulfate/calcium carbonate nanovesicles to realize simultaneous delivery of an anticancer drug and a drug resistance inhibitor into drug-resistant tumor cells...
October 13, 2016: Pharmaceutical Research
Anand A Joshi, Soniya S Vaidya, Marie V St-Pierre, Andrei M Mikheev, Kelly E Desino, Abner N Nyandege, Kenneth L Audus, Jashvant D Unadkat, Phillip M Gerk
The human placenta fulfills a variety of essential functions during prenatal life. Several ABC transporters are expressed in the human placenta, where they play a role in the transport of endogenous compounds and may protect the fetus from exogenous compounds such as therapeutic agents, drugs of abuse, and other xenobiotics. To date, considerable progress has been made toward understanding ABC transporters in the placenta. Recent studies on the expression and functional activities are discussed. This review discusses the placental expression and functional roles of several members of ABC transporter subfamilies B, C, and G including MDR1/P-glycoprotein, the MRPs, and BCRP, respectively...
September 19, 2016: Pharmaceutical Research
Anran Hu, Chen Chen, Michael D Mantle, Bettina Wolf, Lynn F Gladden, Ali Rajabi-Siahboomi, Shahrzad Missaghi, Laura Mason, Colin D Melia
PURPOSE: Investigate the extended release behaviour of compacts containing mixtures of hydrophilic HPMC and PEO in hydrating media of differing ionic strengths. METHODS: The extended release behaviour of various HPMC:PEO compacts was investigated using dissolution testing, confocal microscopy and magnetic resonance imaging, with respect to polymer ratio and ionic strength of the hydrating media. RESULTS: Increasing HPMC content gave longer extended release times, but a greater sensitivity to high ionic dissolution environments...
September 15, 2016: Pharmaceutical Research
Leah C Jimmerson, Lane R Bushman, Michelle L Ray, Peter L Anderson, Jennifer J Kiser
PURPOSE: To develop and validate a method for the simultaneous measurement of adenosine, guanosine, and inosine derived from mono (MP) and triphosphate (TP) forms in peripheral blood mononuclear cells (PBMCs), red blood cells (RBCs) and dried blood spots (DBS). METHODS: Solid phase extraction of cell lysates followed by dephosphorylation to molar equivalent nucleoside and LC-MS/MS quantification. RESULTS: The assay was linear for each of the three quantification ranges: 10-2000, 1...
September 15, 2016: Pharmaceutical Research
Eva M Vicente-Pérez, Helen L Quinn, Emma McAlister, Shannon O'Neill, Lezley-Anne Hanna, Johanne G Barry, Ryan F Donnelly
PURPOSE: To evaluate the combination of a pressure-indicating sensor film with hydrogel-forming microneedle arrays, as a method of feedback to confirm MN insertion in vivo. METHODS: Pilot in vitro insertion studies were conducted using a Texture Analyser to insert MN arrays, coupled with a pressure-indicating sensor film, at varying forces into excised neonatal porcine skin. In vivo studies involved twenty human volunteers, who self-applied two hydrogel-forming MN arrays, one with a pressure-indicating sensor film incorporated and one without...
September 15, 2016: Pharmaceutical Research
Alexandra C Braun, Marcus Gutmann, Regina Ebert, Franz Jakob, Henning Gieseler, Tessa Lühmann, Lorenz Meinel
PURPOSE: The inhibition of myostatin - a member of the transforming growth factor (TGF-β) family - drives regeneration of functional skeletal muscle tissue. We developed a bioresponsive drug delivery system (DDS) linking release of a myostatin inhibitor (MI) to inflammatory flares of myositis to provide self-regulated MI concentration gradients within tissues of need. METHODS: A protease cleavable linker (PCL) - responding to MMP upregulation - is attached to the MI and site-specifically immobilized on microparticle surfaces...
September 14, 2016: Pharmaceutical Research
Walter Schmitt
PURPOSE: To develop an alternative method for estimating vitreal half-lifes in the rabbit eye based on simple equations for the physical processes of dissipation and the physiochemical properties of therapeutic substances applied by intravitreal drug administration. METHODS: Equations were derived to describe diffusion in the vitreous humor and permeation through the back-of-the-eye tissue, and the volume of distribution. The model was validated using reported half-life values from 83 compounds collected from literature...
September 14, 2016: Pharmaceutical Research
Artur Turek, Edyta Olakowska, Aleksandra Borecka, Henryk Janeczek, Michał Sobota, Joanna Jaworska, Bożena Kaczmarczyk, Bożena Jarząbek, Arkadiusz Gruchlik, Marcin Libera, Arkadiusz Liśkiewicz, Halina Jędrzejowska-Szypułka, Janusz Kasperczyk
PURPOSE: Estradiol (E2)-loaded poly(L-lactide-co-glycolide-trimethylenecarbonate) (P(L-LA:GA:TMC)) rods with shape-memory were developed for the treatment of neurodegenerative diseases. Usefulness of the extrusion method in the obtaining process was also considered. The influence of structural and surface properties during hydrolytic degradation was developed. The possible therapeutic aspect of rods with E2 was determined. METHODS: The extruded rods were incubated in a PBS solution (pH 7...
September 14, 2016: Pharmaceutical Research
Francesca Buttini, James Hannon, Kristi Saavedra, Irene Rossi, Anna Giulia Balducci, Hugh Smyth, Andy Clark, Paolo Colombo
PURPOSE: In this work, a novel powder dispersion add-on device, the AOS (Axial Oscillating Sphere), was studied in conjunction with commercially available DPI devices to improve the powder dispersion. METHODS: An ordered mixture of formoterol fumarate and lactose was selected. We studied in two laboratories located at different altitudes the dispensing and dispersion of the drug at different flow rates, paying particular attention to a number of metrics of Fine Particle Dose (FPD)...
September 13, 2016: Pharmaceutical Research
Khurram Rehman, Mohd Hanif Zulfakar
PURPOSE: To characterize bigel system as a topical drug delivery vehicle and to establish the immunomodulatory role of imiquimod-fish oil combination against skin cancer and inflammation resulting from chemical carcinogenesis. METHODS: Imiquimod-loaded fish oil bigel colloidal system was prepared using a blend of carbopol hydrogel and fish oil oleogel. Bigels were first characterized for their mechanical properties and compared to conventional gel systems. Ex vivo permeation studies were performed on murine skin to analyze the ability of the bigels to transport drug across skin and to predict the release mechanism via mathematical modelling...
September 12, 2016: Pharmaceutical Research
Emily E Reichard, Nisha Nanaware-Kharade, Guillermo A Gonzalez, Shraddha Thakkar, S Michael Owens, Eric C Peterson
PURPOSE: Methamphetamine (METH) abuse is a worldwide drug problem, yet no FDA-approved pharmacological treatments are available for METH abuse. Therefore, we produced an anti-METH single chain antibody fragment (scFv7F9Cys) as a pharmacological treatment for METH abuse. ScFv's have a short half-life due to their small size, limiting their clinical use. Thus, we examined the pharmacokinetic effects of conjugating poly(ethylene) glycol (-PEG) to scFv7F9Cys to extend its functional half-life...
September 12, 2016: Pharmaceutical Research
Sean Ekins, Natalie Diaz, Julia Chung, Paul Mathews, Aaron McMurtray
How do we inspire new ideas that could lead to potential treatments for rare or neglected diseases, and allow for serendipity that could help to catalyze them? How many potentially good ideas are lost because they are never tested? What if those ideas could have lead to new therapeutic approaches and major healthcare advances? If a clinician or anyone for that matter, has a new idea they want to test to develop a molecule or therapeutic that they could translate to the clinic, how would they do it without a laboratory or funding? These are not idle theoretical questions but addressing them could have potentially huge economic implications for nations...
September 12, 2016: Pharmaceutical Research
Ayman F El-Kattan, Manthena V Varma, Stefan J Steyn, Dennis O Scott, Tristan S Maurer, Arthur Bergman
PURPOSE: To assess the utility of Extended Clearance Classification System (ECCS) in understanding absorption, distribution, metabolism, and elimination (ADME) attributes and enabling victim drug-drug interaction (DDI) predictions. METHODS: A database of 368 drugs with relevant ADME parameters, main metabolizing enzymes, uptake transporters, efflux transporters, and highest change in exposure (%AUC) in presence of inhibitors was developed using published literature...
September 12, 2016: Pharmaceutical Research
Ni Ai, Richard D Wood, Eric Yang, William J Welsh
PURPOSE: Novel therapeutics are greatly needed that target specific pathological receptors and pathways involved in Neuropathic Pain (NP). Extending our previous work published in this Journal on Group I metabotropic glutamate receptor (mGluR) modulators, we now investigate the therapeutic potential of niclosamide in modulating aberrant glutamate transmission in NP. METHOD: Calcium mobilization assays and cross-receptor selectivity experiments are conducted to characterize the pharmacological activity of niclosamide...
September 8, 2016: Pharmaceutical Research
Ville Vartiainen, Luis M Bimbo, Jouni Hirvonen, Esko I Kauppinen, Janne Raula
PURPOSE: The purpose of this study was to assess the feasibility of hydroxypropyl-β-cyclodextrin as a solubilizer for the corticosteroids prednisolone and fludrocortisone acetate in dry powder inhalation formulations. METHODS: The dry particles were simultaneously produced and coated with nanosized L-leucine crystals using an aerosol flow reactor method. The aerosolization performances of carrier-free powders were studied using Easyhaler® and Twister™ at 2 and 4 kPa pressure drops over the inhalers...
September 7, 2016: Pharmaceutical Research
Marc Lavielle, Benjamin Ribba
PURPOSE: For nonlinear mixed-effects pharmacometric models, diagnostic approaches often rely on individual parameters, also called empirical Bayes estimates (EBEs), estimated through maximizing conditional distributions. When individual data are sparse, the distribution of EBEs can "shrink" towards the same population value, and as a direct consequence, resulting diagnostics can be misleading. METHODS: Instead of maximizing each individual conditional distribution of individual parameters, we propose to randomly sample them in order to obtain values better spread out over the marginal distribution of individual parameters...
September 7, 2016: Pharmaceutical Research
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"