User profiles for Dhiren R. Thakker

Dhiren Thakker

Verified email at unc.edu
Cited by 10697

Enhancing paracellular permeability by modulating epithelial tight junctions

PD Ward, TK Tippin, DR Thakker - Pharmaceutical science & technology …, 2000 - Elsevier
The intestinal epithelium is a major barrier to the absorption of hydrophilic drugs. The presence
of intercellular junctional complexes, particularly the tight junctions (zona occludens), …

Applications of the Caco-2 model in the design and development of orally active drugs: elucidation of biochemical and physical barriers posed by the intestinal …

LSL Gan, DR Thakker - Advanced Drug Delivery Reviews, 1997 - Elsevier
Oral administration is the most important and preferred route of administration for small
molecular weight conventional drugs. The overall bioavailability of an orally administered drug …

Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal …

MD Troutman, DR Thakker - Pharmaceutical research, 2003 - Springer
Purpose. The purpose of this work was to elucidate the asymmetric effect of P-gp on
modulation of absorptive and secretory transport of compounds across polarized epithelium, to …

Mechanisms underlying saturable intestinal absorption of metformin

WR Proctor, DL Bourdet, DR Thakker - Drug Metabolism and Disposition, 2008 - ASPET
The purpose of the study was to elucidate mechanisms of metformin absorptive transport to
explain the dose-dependent absorption observed in humans. Apical (AP) and basolateral (BL…

Efflux ratio cannot assess P-glycoprotein-mediated attenuation of absorptive transport: asymmetric effect of P-glycoprotein on absorptive and secretory transport …

MD Troutman, DR Thakker - Pharmaceutical research, 2003 - Springer
Purpose. The purpose of this work was to determine whether P-glycoprotein (P-gp) modulates
absorptive and secretory transport equally across polarized epithelium (ie, Caco-2 cell …

In vitro hepatic metabolism explains higher clearance of voriconazole in children versus adults: role of CYP2C19 and flavin-containing monooxygenase 3

…, JG Ibrahim, DK Benjamin, DR Thakker - Drug Metabolism and …, 2010 - ASPET
Voriconazole is a broad spectrum antifungal agent for treating life-threatening fungal
infections. Its clearance is approximately 3-fold higher in children compared with adults. …

Four cation-selective transporters contribute to apical uptake and accumulation of metformin in Caco-2 cell monolayers

…, CL Costales, H Cai, RS Everett, DR Thakker - … of Pharmacology and …, 2015 - ASPET
Metformin is the frontline therapy for type II diabetes mellitus. The oral bioavailability of metformin
is unexpectedly high, between 40 and 60%, given its hydrophilicity and positive charge …

Evidence for a polarized efflux system in Caco-2 cells capable of modulating cyclosporine A transport

…, LSL Gan, RW Hendren, DR Thakker - Biochemical and …, 1993 - Elsevier
The characteristics of cyclosporin A (CsA) transport across Caco-2 monolayers were investigated.
CsA (0.25 - 5.0 μM) was transported in a time and concentration dependent manner. …

Organic cation transporter 1 (OCT1/mOct1) is localized in the apical membrane of Caco-2 cell monolayers and enterocytes

…, CM Ng, CL Costales, KLR Brouwer, DR Thakker - Molecular …, 2013 - ASPET
Organic cation transporters (OCTs) are members of the solute carrier 22 family of transporter
proteins that are involved in absorption, distribution, and excretion of organic cations. OCT3 …

Rhodamine 123 requires carrier-mediated influx for its activity as a P-glycoprotein substrate in Caco-2 cells

MD Troutman, DR Thakker - Pharmaceutical research, 2003 - Springer
Purpose. The purpose of this work was to elucidate transport pathways of the P-glycoprotein
(P-gp) substrates rhodamine 123 (R123) and doxorubicin across Caco-2 cells. Methods. …