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Pharmaceutical Research

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https://www.readbyqxmd.com/read/28432535/exploring-the-carbamazepine-interaction-with-human-pregnane-x-receptor-and-effect-on-abcc2-using-in-vitro-and-in-silico-approach
#1
Gurpreet K Grewal, Khuraijam D Singh, Neha Kanojia, Chitra Rawat, Samiksha Kukal, Ajay Jajodia, Anshika Singhal, Richa Misra, Selvaraman Nagamani, Karthikeyan Muthusamy, Ritushree Kukreti
PURPOSE: Over expression of ATP-binding cassette transporters is considered one of the major reasons for non-responsiveness to antiepileptic drugs. Carbamazepine (CBZ), one of first line antiepileptic drug is known to influence ABCC2 expression but its exact molecular mechanism is unknown. METHODS: We investigated the effect of CBZ on expression of ABCC2 and pregnane X receptor (PXR) in HepG2 cell line and compared with hyperforin (agonist of PXR) and ketoconazole (antagonist of PXR) through realtime PCR and western blot assay...
April 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28421307/an-efficient-and-rapid-method-to-monitor-the-oxidative-degradation-of-protein-pharmaceuticals-probing-tyrosine-oxidation-with-fluorogenic-derivatization
#2
Rupesh Bommana, Olivier Mozziconacci, Y John Wang, Christian Schöneich
PURPOSE: The loss of potency of protein therapeutics can be linked to the oxidation of specific amino acid residues leading to a great variety of oxidative modifications. The comprehensive identification of these oxidative modifications requires high-resolution mass spectrometry analysis, which requires time and expensive resources. Here, we propose a fluorogenic derivatization method of oxidized Tyr and Phe yielding benzoxazole derivatives, as an orthogonal technique for the rapid screening of protein oxidation...
April 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28421306/breast-cancer-resistance-protein-and-multidrug-resistance-protein-2-regulate-the-disposition-of-acacetin-glucuronides
#3
Huangyu Jiang, Jia Yu, Haihui Zheng, Jiamei Chen, Jinjun Wu, Xiaoxiao Qi, Ying Wang, Xinchun Wang, Ming Hu, Lijun Zhu, Zhongqiu Liu
PURPOSE: To determine the mechanism responsible for acacetin glucuronide transport and the bioavailability of acacetin. METHODS: Area under the curve (AUC), clearance (CL), half-life (T1/2) and other pharmacokinetic parameters were determined by the pharmacokinetic model. The excretion of acacetin glucuronides was evaluated by the mouse intestinal perfusion model and the Caco-2 cell model. RESULTS: In pharmacokinetic studies, the bioavailability of acacetin in FVB mice was 1...
April 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28409325/velocity-field-visualization-in-usp-dissolution-apparatus-3-using-particle-image-velocimetry
#4
Satish Perivilli, Richard Prevost, Erika Stippler
PURPOSE: The hydrodynamics in USP dissolution apparatus 3, at five different dip rates, was characterized by analyzing phase-averaged velocity fields obtained using Particle Image Velocimetry (PIV). METHODS: Phase locked 2 Component-PIV (2C-PIV) measurements were recorded on a typical dissolution apparatus 3 configuration with a black painted tablet fixed at the center of the bottom porous screen of the reciprocating cylinder. A trigger mechanism was employed to capture data over 12 phase positions for each reciprocation cycle...
April 13, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28405914/cyclosporine-a-loaded-electrospun-poly-d-l-lactic-acid-poly-ethylene-glycol-nanofibers-drug-carriers-utilizable-in-local-immunosuppression
#5
Jakub Sirc, Zuzana Hampejsova, Jana Trnovska, Petr Kozlik, Jakub Hrib, Radka Hobzova, Alena Zajicova, Vladimir Holan, Zuzana Bosakova
PURPOSE: The present study aims to prepare poly(D,L-lactic acid) (PLA) nanofibers loaded by the immunosuppressant cyclosporine A (CsA, 10 wt%). Amphiphilic poly(ethylene glycol)s (PEG) additives were used to modify the hydrophobic drug release kinetics. METHODS: Four types of CsA-loaded PLA nanofibrous carriers varying in the presence and molecular weight (MW) of PEG (6, 20 and 35 kDa) were prepared by needleless electrospinning. The samples were extracted for 144 h in phosphate buffer saline or tissue culture medium...
April 12, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28405913/in-vitro-transport-activity-and-trafficking-of-mrp2-abcc2-polymorphic-variants
#6
Xia Wen, Melanie S Joy, Lauren M Aleksunes
PURPOSE: Multidrug resistance-associated protein 2 (MRP2/ABCC2) is an efflux pump that removes drugs and chemicals from cells. We sought to characterize the expression, trafficking and in vitro activity of seven single nucleotide polymorphisms (SNPs) in the ABCC2 gene. METHODS: ABCC2 SNPs were generated using site-directed mutagenesis and stably expressed in Flp-In HEK293 cells, which allows targeted insertion of transgenes within the genome. Total and cell surface expression of MRP2 as well as accumulation of substrates (calcein AM and 5(6)-carboxy-2',7'-dichlorofluorescein diacetate, CDCF) were quantified in cells or inverted membrane vesicles expressing wild-type (WT) or variant forms...
April 12, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28405912/continuous-transdermal-delivery-of-l-dopa-based-on-a-self-assembling-nanomicellar-system
#7
Amnon C Sintov, Haim V Levy, Igor Greenberg
PURPOSE: When levodopa (L-DOPA) is administered orally, it is eliminated from the body very quickly resulting in a series of sharp fluctuations in its blood concentrations. These frequent changes in blood levels are considered to be responsible for the development of late motor complications and dyskinesias, which are troubling clinical and treatment issues in Parkinson's disease. Transdermal drug delivery is a patient-compliant method for delivering therapeutics into the systemic circulation in a continuous and controlled manner...
April 12, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28401430/bilateral-effects-of-excipients-on-protein-stability-preferential-interaction-type-of-excipient-and-surface-aromatic-hydrophobicity-of-protein
#8
Lili Wen, Xianxian Zheng, Xinyue Wang, Hairong Lan, Zongning Yin
PURPOSE: Understanding the mechanism of protein-excipient interaction and illuminating the influencing factors on protein stability are key steps in the rational design of protein formulations. The objective of this study was to assess effects of preferential interaction type of excipient and surface aromatic hydrophobicity of protein on protein solution stability. METHODS: The preferential interaction between excipient and aromatic hydrophobic area of protein was investigated by solubility and fluorescence studies of amino acid derivatives in excipient solutions...
April 11, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28397089/virtual-clinical-studies-to-examine-the-probability-distribution-of-the-auc-at-target-tissues-using-physiologically-based-pharmacokinetic-modeling-application-to-analyses-of-the-effect-of-genetic-polymorphism-of-enzymes-and-transporters-on-irinotecan-induced
#9
Kota Toshimoto, Atsuko Tomaru, Masakiyo Hosokawa, Yuichi Sugiyama
PURPOSE: To establish a physiologically-based pharmacokinetic (PBPK) model for analyzing the factors associated with side effects of irinotecan by using a computer-based virtual clinical study (VCS) because many controversial associations between various genetic polymorphisms and side effects of irinotecan have been reported. METHODS: To optimize biochemical parameters of irinotecan and its metabolites in the PBPK modeling, a Cluster Newton method was introduced...
April 10, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28389708/mathematical-modeling-and-experimental-validation-of-nanoemulsion-based-drug-transport-across-cellular-barriers
#10
Ekta Kadakia, Lipa Shah, Mansoor M Amiji
PURPOSE: Nanoemulsions have shown potential in delivering drug across epithelial and endothelial cell barriers, which express efflux transporters. However, their transport mechanisms are not entirely understood. Our goal was to investigate the cellular permeability of nanoemulsion-encapsulated drugs and apply mathematical modeling to elucidate transport mechanisms and sensitive nanoemulsion attributes. METHODS: Transport studies were performed in Caco-2 cells, using fish oil nanoemulsions and a model substrate, rhodamine-123...
April 7, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28389707/the-race-of-10-synthetic-rnai-based-drugs-to-the-pharmaceutical-market
#11
REVIEW
Ricardo Titze-de-Almeida, Catherine David, Simoneide Souza Titze-de-Almeida
Ten years after Fire and Melo's Nobel Prize for discovery of gene silencing by double-stranded RNA, a remarkable progress was achieved in RNA interference (RNAi). Changes in the chemical structure of synthetic oligonucleotides make them more stable and specific, and new delivery strategies became progressively available. The attention of pharmaceutical industry rapidly turned to RNAi, as an opportunity to explore new drug targets. This review addresses nine small-interfering RNAs (siRNAs) and one unique microRNA (miRNA) inhibitor, which entered the phase 2-3 clinical trials...
April 7, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28386634/insights-and-lessons-from-a-scientific-conference-on-non-invasive-delivery-of-macromolecules
#12
Ronak Savla, Randall J Mrsny, Kinam Park, Isabelle Aubert, Cornell Stamoran
A growing share of the pharmaceutical development pipeline is occupied by macromolecule drugs, which are primarily administered by injection. Despite decades of attempts, non-invasive delivery of macromolecules has seen only a few success stories. Potential benefits of non-invasive administration include better patient acceptance and adherence and potentially better efficacy and safety. Greater inter-disciplinary dialogue and collaboration are integral to realizing these benefits.
April 6, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28386633/rlip76-inhibition-a-promising-developmental-therapy-for-neuroblastoma
#13
REVIEW
Sharad S Singhal, Lokesh Nagaprashantha, Preeti Singhal, Sulabh Singhal, Jyotsana Singhal, Sanjay Awasthi, David Horne
Refractory and relapsed neuroblastoma (NB) present with significant challenges in clinical management. Though primary NBs largely with wild-type p53 respond well to interventions, dysfunctional signaling in the p53 pathways in a MYCN oncogene driven background is found in a number of children with NB. The p53-mutant NB is largely unresponsive to available therapies and p53-independent targeted therapeutics represents a vital need in pediatric oncology. We analyzed the findings on mercapturic acid pathway (MAP) transporter RLIP76, which has broad and critical effects on multiple pathways as essential for carcinogenesis, oxidative stress and drug-resistance, is over-expressed in NB...
April 6, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28382563/formulation-of-a-sustained-release-docetaxel-loaded-cockle-shell-derived-calcium-carbonate-nanoparticles-against-breast-cancer
#14
Nahidah Ibrahim Hammadi, Yusuf Abba, Mohd Noor Mohd Hezmee, Intan Shameha Abdul Razak, Alhaji Zubair Jaji, Tijani Isa, Saffanah Khuder Mahmood, Md Zuki Abu Bakar Zakaria
PURPOSE: Here, we explored the formulation of a calcium carbonate nanoparticle delivery system aimed at enhancing docetaxel (DTX) release in breast cancer. METHODS: The designed nano- anticancer formulation was characterized thorough X-ray diffraction (XRD), Fourier transformed infrared (FTIR), transmission electron microscopy (TEM) and field emission scanning electron microscopy (FESEM) and Brunauer-Emmett-Teller (BET) methods. The nano- anticancer formulation (DTX- CaCO3NP) was evaluated for drug delivery properties thorough in vitro release study in human body simulated solution at pH 7...
April 5, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28374339/structure-function-analysis-of-phenylpiperazine-derivatives-as-intestinal-permeation-enhancers
#15
Katherine C Fein, Nicholas G Lamson, Kathryn A Whitehead
PURPOSE: A major obstacle preventing oral administration of macromolecular therapeutics is poor absorption across the intestinal epithelium into the bloodstream. One strategy to improve transport across this barrier is the use of chemical permeation enhancers. Several molecular families with permeation enhancing potential have been identified previously, including piperazines. In particular, 1-phenylpiperazine has been shown to enhance transepithelial transport with minimal cytotoxicity compared to similarly effective molecules...
April 3, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28374338/therapeutic-drug-monitoring-of-golimumab-in-the-treatment-of-ulcerative-colitis
#16
REVIEW
Niels Vande Casteele, Reena Khanna
Ulcerative colitis (UC) is a relapsing-remitting chronic inflammatory disorder affecting the mucosal surface in a continuous manner from the rectum through part of, or the entire, colon. Patients with severe disease and those who become refractory or intolerant to corticosteroids and/or immunosuppressants, require treatment with biologic agents that target tumor necrosis factor-α (TNF). Golimumab, a fully human monoclonal antibody, is the latest TNF antagonist to get approved for the treatment of moderate-to-severe UC...
April 3, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28364304/inter-subject-variability-in-oct1-activity-in-27-batches-of-cryopreserved-human-hepatocytes-and-association-with-oct1-mrna-expression-and-genotype
#17
Sarinj Fattah, Abhijit Babaji Shinde, Maja Matic, Myriam Baes, Ron H N van Schaik, Karel Allegaert, Celine Parmentier, Lysiane Richert, Patrick Augustijns, Pieter Annaert
PURPOSE: OCT1/3 (Organic Cation Transporter-1 and -3; SLC22A1/3) are transmembrane proteins localized at the basolateral membrane of hepatocytes. They mediate the uptake of cationic endogenous compounds and/or xenobiotics. The present study was set up to verify whether the previously observed variability in OCT activity in hepatocytes may be explained by inter-individual differences in OCT1/3 mRNA levels or OCT1 genotype. METHODS: Twenty-seven batches of cryopreserved human hepatocytes (male and female, age 24-88 y) were characterized for OCT activity, normalized OCT1/3 mRNA expression, and OCT1 genetic mutation...
March 31, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28361200/utilization-of-liver-microsomes-to-estimate-hepatic-intrinsic-clearance-of-monoamine-oxidase-substrate-drugs-in-humans
#18
Yusuke Masuo, Shushi Nagamori, Aoi Hasegawa, Kazuki Hayashi, Noriyoshi Isozumi, Noritaka Nakamichi, Yoshikatsu Kanai, Yukio Kato
PURPOSE: Monoamine oxidases (MAOs) are non-CYP enzymes that contribute to systemic elimination of therapeutic agents, and localized on mitochondrial membranes. The aim of the present study was to validate quantitative estimation of metabolic clearance of MAO substrate drugs using human liver microsomes (HLMs). METHODS: Three MAO substrate drugs, sumatriptan, rizatriptan and phenylephrine, as well as four CYP substrates were selected, and their disappearance during incubation with HLMs or mitochondria (HLMt) was measured...
March 30, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28352994/impact-of-micellar-surfactant-on-supersaturation-and-insight-into-solubilization-mechanisms-in-supersaturated-solutions-of-atazanavir
#19
Anura S Indulkar, Huaping Mo, Yi Gao, Shweta A Raina, Geoff G Z Zhang, Lynne S Taylor
PURPOSE: The goals of this study were to determine: 1) the impact of surfactants on the "amorphous solubility"; 2) the thermodynamic supersaturation in the presence of surfactant micelles; 3) the mechanism of solute solubilization by surfactant micelles in supersaturated solutions. METHODS: The crystalline and amorphous solubility of atazanavir was determined in the presence of varying concentrations of micellar sodium dodecyl sulfate (SDS). Flux measurements, using a side-by-side diffusion cell, were employed to determine the free and micellar-bound drug concentrations...
March 28, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28352993/preclinical-evaluation-of-the-short-term-toxicity-of-4-n-docosahexaenoyl-2%C3%A2-2%C3%A2-difluorodeoxycytidine-dha-dfdc
#20
Solange Valdes, Youssef W Naguib, Rick A Finch, Wallace B Baze, Christopher A Jolly, Zhengrong Cui
PURPOSE: This study was designed to test the short-term toxicity of DHA-dFdC in a mouse model and its efficacy in a mouse model of leukemia at or below its repeat-dose maximum tolerated dose (RD-MTD). METHOD: A repeat-dose dose-ranging toxicity study was designed to determine the tolerability of DHA-dFdC when administered to DBA/2 mice by intravenous (i.v.) injection on a repeat-dose schedule (i.e. injections on days 0, 3, 7, 10, and 13). In order to determine the effect of a lethal dose of DHA-dFdC, mice were injected i...
March 28, 2017: Pharmaceutical Research
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