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Pharmaceutical Research

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https://www.readbyqxmd.com/read/28101809/sequential-exposure-of-bortezomib-and-vorinostat-is-synergistic-in-multiple-myeloma-cells
#1
Charvi Nanavati, Donald E Mager
PURPOSE: To examine the combination of bortezomib and vorinostat in multiple myeloma cells (U266) and xenografts, and to assess the nature of their potential interactions with semi-mechanistic pharmacodynamic models and biomarkers. METHODS: U266 proliferation was examined for a range of bortezomib and vorinostat exposure times and concentrations (alone and in combination). A non-competitive interaction model was used with interaction parameters that reflect the nature of drug interactions after simultaneous and sequential exposures...
January 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28097509/revealing-pmdi-spray-initial-conditions-flashing-atomisation-and-the-effect-of-ethanol
#2
Nicholas Mason-Smith, Daniel J Duke, Alan L Kastengren, Daniela Traini, Paul M Young, Yang Chen, David A Lewis, Daniel Edgington-Mitchell, Damon Honnery
PURPOSE: Sprays from pressurised metered-dose inhalers are produced by a transient discharge of a multiphase mixture. Small length and short time scales have made the investigation of the governing processes difficult. Consequently, a deep understanding of the physical processes that govern atomisation and drug particle formation has been elusive. METHODS: X-ray phase contrast imaging and quantitative radiography were used to reveal the internal flow structure and measure the time-variant nozzle exit mass density of 50 µL metered sprays of HFA134a, with and without ethanol cosolvent...
January 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28097508/preparation-and-evaluation-of-biopolymeric-nanoparticles-as-drug-delivery-system-in-effective-treatment-of-rheumatoid-arthritis
#3
Vijay Kumar, Ankita Leekha, Aakriti Tyagi, Ankur Kaul, Anil Kumar Mishra, Anita Kamra Verma
PURPOSE: The study purposes to evaluate nanocrystalline biopolymeric nanoparticles encapsulating methotrexate and dexamethasone with high biocompatibility, enhanced therapeutic efficacy and reduced toxicity. METHODS: Chitosan nanoparticles were prepared by ionic gelation, and Methotrexate (MTX) and Dexamethasone (DEX) were loaded during the preparation and screened for their in vitro efficacy in HEK and RAW264.7 cells, ex vivo and in vivo efficacy. RESULTS: FTIR confirmed the involvement of phosphoric group of sTPP with amine groups of chitosan and also role of hydrogen bonding involved in the preparation of MTXCHNP and DEXCHNP...
January 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28097507/in-vitro-phase-i-and-phase-ii-drug-metabolism-in-the-liver-of-juvenile-and-adult-g%C3%A3-ttingen-minipigs
#4
Els Van Peer, Frank Jacobs, Jan Snoeys, Jos Van Houdt, Ils Pijpers, Christophe Casteleyn, Chris Van Ginneken, Steven Van Cruchten
PURPOSE: In view of pediatric drug development, juvenile animal studies are gaining importance. However, data on drug metabolizing capacities of juvenile animals are scarce, especially in non-rodent species. Therefore, we aimed to characterize the in vitro biotransformation of four human CYP450 substrates and one UGT substrate in the livers of developing Göttingen minipigs. METHODS: Liver microsomes from late fetal, Day 1, Day 3, Day 7, Day 28, and adult male and female Göttingen minipigs were incubated with a cocktail of CYP450 substrates, including phenacetin, tolbutamide, dextromethorphan, and midazolam...
January 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28097506/bioequivalence-methodologies-for-topical-drug-products-in-vitro-and-ex-vivo-studies-with-a-corticosteroid-and-an-anti-fungal-drug
#5
Leila Bastos Leal, Sarah F Cordery, M Begoña Delgado-Charro, Annette L Bunge, Richard H Guy
OBJECTIVE: To examine whether in vitro and ex vivo measurements of topical drug product performance correlate with in vivo outcomes, such that more efficient experimental approaches can be reliably and reproducibly used to establish (in)equivalence between formulations for skin application. MATERIALS AND METHODS: In vitro drug release through artificial membranes, and drug penetration into porcine skin ex vivo, were compared with published human in vivo studies...
January 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28078484/the-effect-of-surface-charges-on-the-cellular-uptake-of-liposomes-investigated-by-live-cell-imaging
#6
Ji Hee Kang, Woo Young Jang, Young Tag Ko
PURPOSE: Liposomes have been developed as versatile nanocarriers for various pharmacological agents. The effect of surface charges on the cellular uptake of the liposomes has been studied by various methods using mainly fixed cells with inevitable limitations. Live cell imaging has been proposed as an alternative methods to overcome the limitations of the fixed cell-based analysis. In this study, we aimed to investigate the effects of surface charges on cellular association and internalization of the liposomes using live cell imaging...
January 11, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28074431/detection-and-specific-elimination-of-egfr-ovarian-cancer-cells-using-a-near-infrared-photoimmunotheranostic-approach
#7
Dirk Bauerschlag, Ivo Meinhold-Heerlein, Nicolai Maass, Andreas Bleilevens, Karen Bräutigam, Wa'el Al Rawashdeh, Stefano Di Fiore, Anke Maria Haugg, Felix Gremse, Julia Steitz, Rainer Fischer, Elmar Stickeler, Stefan Barth, Ahmad Fawzi Hussain
PURPOSE: Targeted theranostics is an alternative strategy in cancer management that aims to improve cancer detection and treatment simultaneously. This approach combines potent therapeutic and diagnostic agents with the specificity of different cell receptor ligands in one product. The success of antibody drug conjugates (ADCs) in clinical practice has encouraged the development of antibody theranostics conjugates (ATCs). However, the generation of homogeneous and pharmaceutically-acceptable ATCs remains a major challenge...
January 10, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28070753/dodecyl-amino-glucoside-enhances-transdermal-and-topical-drug-delivery-via-reversible-interaction-with-skin-barrier-lipids
#8
Monika Kopečná, Miloslav Macháček, Eva Prchalová, Petr Štěpánek, Pavel Drašar, Martin Kotora, Kateřina Vávrová
PURPOSE: Skin permeation/penetration enhancers are substances that enable drug delivery through or into the skin. METHODS: To search for new enhancers with high but reversible activity and acceptable toxicity, we synthesized a series of D-glucose derivatives, both hydrophilic and amphiphilic. RESULTS: Initial evaluation of the ability of these sugar derivatives to increase permeation and penetration of theophylline through/into human skin compared with a control (no enhancer) or sorbitan monolaurate (Span 20; positive control) revealed dodecyl 6-amino-6-deoxy-α-D-glucopyranoside 5 as a promising enhancer...
January 9, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28035628/effects-of-histidine-and-sucrose-on-the-biophysical-properties-of-a-monoclonal-antibody
#9
Youngbin Baek, Nripen Singh, Abhiram Arunkumar, Andrew L Zydney
PURPOSE: Histidine is a commonly used buffer in formulation of monoclonal antibodies (mAb), often with excipients like sucrose. The objective of this study was to examine the effects of both histidine and sucrose on the biophysical characteristics of a mAb. METHODS: The hydrodynamic radius of the mAb was determined by dynamic light scattering and confirmed by size exclusion chromatography. Data were also obtained for the osmotic virial coefficients (from osmotic pressure measurements), the solution viscosity, and the mAb thermal stability (using differential scanning calorimetry) at selected conditions...
December 29, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28035627/supramolecular-cocrystals-of-gliclazide-synthesis-characterization-and-evaluation
#10
Renu Chadha, Dimpy Rani, Parnika Goyal
PURPOSE: To prepare the supramolecular cocrystals of gliclazide (GL, a BCS class II drug molecule) via mechanochemical route, with the goal of improving physicochemical and biopharmaceutical properties. METHODS: Two cocrystals of GL with GRAS status coformers, sebacic acid (GL-SB; 1:1) and α-hydroxyacetic acid (GL-HA; 1:1) were screened out using liquid assisted grinding. The prepared cocrystals were characterized using thermal and analytical techniques followed by evaluation of antidiabetic activity and pharmacokinetic parameters...
December 29, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28028771/modeling-the-effect-of-the-selective-s1p1-receptor-modulator-ponesimod-on-subsets-of-blood-lymphocytes
#11
Dominik Lott, Andreas Krause, Christian A Seemayer, Daniel S Strasser, Jasper Dingemanse, Thorsten Lehr
PURPOSE: This analysis aimed at describing the effect of the selective sphingosine-1-phosphate receptor 1 modulator ponesimod on lymphocyte subsets in peripheral blood. As the involvement of different lymphocyte subsets varies among different autoimmune diseases, characterizing the effect of ponesimod on these may be beneficial in better understanding treatment effects. METHODS: Three phase 1 clinical studies in healthy human subjects were pooled. Non-linear mixed-effects modeling techniques were used to study the effect of ponesimod on lymphocyte subsets such as B cells, T helper cells, T cytotoxic cells, and natural killer cells in a qualitative and quantitative manner...
December 27, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28028770/on-the-nature-of-physiologically-based-pharmacokinetic-models-a-priori-or-a-posteriori-mechanistic-or-empirical
#12
Ken Korzekwa, Swati Nagar
Physiologically-based pharmacokinetic (PBPK) models explicitly incorporate tissue-specific blood flows, partition coefficients, and metabolic processes. Since PBPK models are derived using physiologic parameters and interactions of the compound with tissue components, these models are considered to be "bottom up" as opposed to "top down". Modeling approaches can be characterized as either a posteriori (observational) or a priori (based solely on theory). Furthermore, approaches can be mechanistic (structure and components based on mechanisms) or empirical (based on observations alone)...
December 27, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28028769/are-polymorphisms-in-genes-relevant-to-drug-disposition-predictors-of-susceptibility-to-drug-induced-liver-injury
#13
Ann K Daly
Despite considerable progress in identifying specific HLA alleles as genetic risk factors for some forms of drug-induced liver injury, progress in understanding whether genetic polymorphisms relevant to drug disposition also contribute to risk for developing this serious toxicity has been more limited. Evidence from both candidate-gene case control studies and genome-wide association studies is now discussed. In the case of genes relevant to drug metabolism, polymorphisms in cytochromes P450, UDP-glucuronosyltransferases, N-acetyltransferases and glutathione S-transferases as risk factors for DILI are assessed...
December 27, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28028768/meal-effects-confound-attempts-to-counteract-rabeprazole-induced-hypochlorhydria-decreases-in-atazanavir-absorption
#14
Kathleen Panter Faber, Hsin-Fang Wu, Marc R Yago, Xiaohui Xu, Pathanjali Kadiyala, Lynda A Frassetto, Leslie Z Benet
PURPOSE: Clinically relevant pharmacokinetic interactions exist between gastric acid-reducing agents and certain weakly basic drugs that rely on acidic environments for optimal oral absorption. In this study, we examine whether the administration of betaine hydrochloride under fed conditions can enhance the absorption of atazanavir, an HIV-1 protease inhibitor, during pharmacologically-induced hypochlorhydria. METHODS: In this randomized, single-dose, 3 period, crossover study healthy volunteers received ritonavir-boosted atazanavir (atazanavir/ritonavir 300/100 mg) alone, following pretreatment with the proton pump inhibitor rabeprazole (20 mg twice daily), and with 1500 mg of betaine HCl after rabeprazole pretreatment...
December 27, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28004318/analysis-of-3d-prints-by-x-ray-computed-microtomography-and%C3%A2-terahertz-pulsed-imaging
#15
Daniel Markl, J Axel Zeitler, Cecilie Rasch, Maria Høtoft Michaelsen, Anette Müllertz, Jukka Rantanen, Thomas Rades, Johan Bøtker
PURPOSE: A 3D printer was used to realise compartmental dosage forms containing multiple active pharmaceutical ingredient (API) formulations. This work demonstrates the microstructural characterisation of 3D printed solid dosage forms using X-ray computed microtomography (XμCT) and terahertz pulsed imaging (TPI). METHODS: Printing was performed with either polyvinyl alcohol (PVA) or polylactic acid (PLA). The structures were examined by XμCT and TPI. Liquid self-nanoemulsifying drug delivery system (SNEDDS) formulations containing saquinavir and halofantrine were incorporated into the 3D printed compartmentalised structures and in vitro drug release determined...
December 21, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28004317/biodegradable-polymersomes-as-nanocarriers-for-doxorubicin-hydrochloride-enhanced-cytotoxicity-in-mcf-7-adr-cells-and-prolonged-blood-circulation
#16
Yanhui Chao, Yuheng Liang, Guihua Fang, Haibing He, Qing Yao, Hang Xu, Yinrong Chen, Xing Tang
PURPOSE: DOX is one of the most potent anticancer drugs. But its short half-life and the occurrence of multi-drug resistance (MDR) markedly limit its clinical application. To solve these problems, we develop DOX loaded polymersomes (DOX polymersomes). METHODS: An methoxy poly(ethylene glycol)-b-poly(epsilon-caprolactone) (mPEG-b-PCL) copolymer was synthesized and used to prepare DOX polymersomes. The pharmaceutical properties of DOX polymersomes were characterized...
December 21, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28004316/denatured-whey-protein-powder-as-a-new-matrix-excipient-design-and-evaluation-of-mucoadhesive-tablets-for-sustained-drug-release-applications
#17
Hassana Hsein, Ghislain Garrait, Fahima Tamani, Eric Beyssac, Valérie Hoffart
PURPOSE: In earlier study, we proposed denatured whey protein (DWP) powder obtained by atomization as a new excipient to promote oral drug delivery. In this work, we evaluate the possibility to formulate tablets based on DWP powders and to characterize their role as a matrix mucoadhesive excipient. METHODS: Tablets containing increased amount of DWP (10 to 30%) were produced by direct compression after mixing with theophylline, microcrystalline cellulose, Aerosil® and magnesium stearate...
December 21, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28004315/bioflavonoid-fisetin-loaded-%C3%AE-tocopherol-poly-lactic-acid-based-polymeric-micelles-for-enhanced-anticancer-efficacy-in-breast-cancers
#18
Lei Wang, De-Zhong Zhang, Yu-Xia Wang
PURPOSE: In this study, tocopherol based polymeric micelles were successfully prepared to enhance the anticancer effect of fisetin (FIS) in breast cancer cells. METHODS: The drug-loaded carrier was characterized in terms of physicochemical and in vivo parameters. RESULTS: Compared to FIS, FIS-TPN showed higher cellular uptake in MCF-7 breast cancer cells as revealed by CLSM and flow cytometry. The cytotoxicity assay results clearly showed that the free FIS and FIS-TPN exhibited a typical dose-dependent toxic effect in MCF-7 breast cancer cells...
December 21, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27995525/pharmacokinetics-and-biodistribution-of-gdc-0449-loaded-micelles-in-normal-and-liver-fibrotic-mice
#19
Rinku Dutta, Virender Kumar, Yang Peng, Ruby E Evande, Jean L Grem, Ram I Mahato
PURPOSES: To determine the pharmacokinetic parameters and biodistribution of GDC-0449 loaded polymeric micelles after systemic administration into common bile duct ligation (CBDL) induced liver fibrotic mice. METHODS: We used GDC-0449 encapsulated methoxy poly (ethylene glycol)-block-poly (2-methyl-2-carboxyl-propylene carbonate)-graft-dodecanol (PEG-PCD) non-targeted polymeric micelles for GDC-0449 delivery to normal and liver fibrotic mice. To maximize GDC-0449 delivery to hepatic stellate cells (HSCs), mixed micelles formulations with 10, 20 and 30% w/w mannose-6-phosphate (M6P)-conjugated micelles were administered to normal and liver fibrotic mice for targeting M6P/IGF-IIR overexpressed on activated HSCs and biodistribution of GDC-0449 was determined at 30 and 120 min post systemic administration...
December 19, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27995524/intra-and-extracellular-biosynthesis-and-characterization-of-iron-nanoparticles-from-prokaryotic-microorganisms-with-anticoagulant-activity
#20
Karina A Crespo, José L Baronetti, Melisa A Quinteros, Paulina L Páez, María G Paraje
BACKGROUND: The use of microorganisms for the synthesis of nanoparticles (NPs) is relatively new in basic research and technology areas. PURPOSE: This work was conducted to optimized the biosynthesis of iron NPs intra- and extracellular by Escherichia coli or Pseudomonas aeruginosa and to evaluate their anticoagulant activity. STUDY DESIGN/METHODS: The structures and properties of the iron NPs were investigated by Ultraviolet-visible (UV-vis) spectroscopy, Zeta potential, Dynamic light scattering (DLS), Field emission scanning electron microscope (FESEM)/ Energy dispersive X-ray (EDX) and transmission electron microscopy (TEM)...
December 19, 2016: Pharmaceutical Research
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