Online citations, reference lists, and bibliographies.
← Back to Search

Polarized Transport Of Docetaxel And Vinblastine Mediated By P-glycoprotein In Human Intestinal Epithelial Cell Monolayers.

P. Wils, V. Phung-Ba, A. Warnery, D. Lechardeur, S. Raeissi, I. Hidalgo, D. Scherman
Published 1994 · Biology, Medicine

Save to my Library
Download PDF
Analyze on Scholarcy Visualize in Litmaps
Reduce the time it takes to create your bibliography by a factor of 10 by using the world’s favourite reference manager
Time to take this seriously.
Get Citationsy
The expression of the multidrug transporter P-glycoprotein has been studied in two human intestinal epithelial cell lines. No functional expression of P-glycoprotein was found in the differentiated HT29-18-C1 cell line. The expression of P-glycoprotein in the Caco-2 cell line was very high, as judged by immunoblotting and by active efflux of vinblastine. The polarized transport of vinblastine in the basolateral to apical direction was temperature and energy dependent, and was reduced by P-glycoprotein inhibitors such as verapamil, chlorpromazine and reserpine. This adds further evidence that the polarized transport of vinblastine across Caco-2 monolayers is mediated by P-glycoprotein. The anticancer drug docetaxel (Taxotere) was transported in a polarized manner: basolateral to apical permeability was 20-fold higher than in the reverse direction. This polarized transport was inhibited by verapamil, chlorpromazine and reserpine, thus demonstrating that docetaxel is a substrate of P-glycoprotein. The implications of these results for the pharmacokinetics and toxicity of taxoids are discussed.
This paper references
Absorptive and mucus-secreting subclones isolated from a multipotent intestinal cell line (HT-29) provide new models for cell polarity and terminal differentiation
C. Huet (1987)
Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues.
F. Thiebaut (1987)
ATP-dependent transport of vinblastine in vesicles from human multidrug-resistant cells.
M. Horio (1988)
Purification of the 170- to 180-kilodalton membrane glycoprotein associated with multidrug resistance. 170- to 180-kilodalton membrane glycoprotein is an ATPase.
H. Hamada (1988)
Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites.
C. Cordon-Cardo (1989)
Modulation by verapamil of vincristine pharmacokinetics and sensitivity to metaphase arrest of the normal rat colon in organ culture.
P. Ince (1991)
Studies with RP 56976 (taxotere): a semisynthetic analogue of taxol.
I. Ringel (1991)
Biochemical characterization of resistance to mitoxantrone and adriamycin in Caco-2 human colon adenocarcinoma cells: a possible role for glutathione S-transferases.
W. Peters (1992)
Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators.
J. Hunter (1993)
HT29-18-C1 intestinal cells: a new model for studying the epithelial transport of drugs.
P. Wils (1993)
High lipophilicity decreases drug transport across intestinal epithelial cells.
P. Wils (1994)

This paper is referenced by
Docetaxel/dimethyl-β-cyclodextrin inclusion complexes: preparation, in vitro evaluation and physicochemical characterization
Bhupendra Raj Giri (2021)
ADME gene polymorphisms do not influence the pharmacokinetics of docetaxel: Results from a population pharmacokinetic study in Indian cancer patients
A. Patil (2021)
P-Glycoprotein-Mediated Efflux Using a Rapidly Maturing Caco2 Clone (CLEFF4) in Only 5 Days without Requiring Modified Growth Medium
A. Crowe (2020)
ABC Transporters in Extrahepatic Tissues: Pharmacological Regulation in Heart and Intestine.
S. Villanueva (2019)
How to overcome ATP-binding cassette drug efflux transporter-mediated drug resistance?
Carolina Mantilla (2018)
Preparation, characterization, and pharmacokinetics of liposomal docetaxel for oral administration
J. Kim (2018)
Development of RP-HPLC method for simultaneous determination of docetaxel and curcumin in rat plasma: Validation and stability
D. W. Kim (2017)
Clinical Implications of P-Glycoprotein Modulation in Drug–Drug Interactions
M. Lund (2017)
Renal Drug Transporters and Drug Interactions
A. Ivanyuk (2017)
Synthesis and in vitro Biological Evaluation of Ferrocenyl Side‐Chain‐Functionalized Paclitaxel Derivatives
D. Plażuk (2017)
The role of membrane transporters in ovarian cancer chemoresistance and prognosis
Ela Cerovská (2017)
Preparation and characterization of docetaxel self-nanoemulsifying powders (SNEPs): A strategy for improved oral delivery
Sharath Sunkavalli (2016)
Population pharmacokinetic–pharmacodynamic modeling and model-based prediction of docetaxel-induced neutropenia in Japanese patients with non-small cell lung cancer
Masato Fukae (2016)
Acquisition of anticancer drug resistance is partially associated with cancer stemness in human colon cancer cells.
Flaria El Khoury (2016)
Pharmacological and Interventional Approaches for Optimizing Taxane Treatment
Annemieke J. M. Nieuweboer (2016)
New Oral Formulation and in Vitro Evaluation of Docetaxel-Loaded Nanomicelles
A. Hekmat (2016)
Prognostic Value and Implication for Chemotherapy Treatment of ABCB1 in Epithelial Ovarian Cancer: A Meta-Analysis
Si Sun (2016)
Development and evaluation of curcumin-loaded Pluronic F127 nanoformulation
S. Shamsi (2015)
Emerging chemotherapy agents in lung cancer: nanoparticles therapeutics for non-small cell lung cancer
G. In (2015)
The role of ABC transporters in ovarian cancer progression and chemoresistance.
M. Ween (2015)
Docetaxel Induced Sclerosing Cholangitis
J. Horsley-Silva (2015)
Inter-patient variability in docetaxel pharmacokinetics: A review.
A. Nieuweboer (2015)
Contribution of Hepatic Organic Anion-Transporting Polypeptides to Docetaxel Uptake and Clearance
Hannah H Lee (2015)
BRCA2-deficient sarcomatoid mammary tumors exhibit multidrug resistance.
J. Jaspers (2015)
Preparation and evaluation in vitro and in vivo of docetaxel loaded mixed micelles for oral administration.
J. Dou (2014)
Nanotechnology based approaches in cancer therapeutics
A. Biswas (2014)
Combination antiretroviral therapy (cART) component ritonavir significantly alters docetaxel exposure
M. Rudek (2014)
Pharmacogenetics of membrane transporters: a review of current approaches.
T. Sissung (2014)
Pregnane X Receptor and P-glycoprotein: a connexion for Alzheimer’s disease management
Sumit Jain (2014)
J. Lorbeer (2014)
The limited intestinal absorption via paracellular pathway is responsible for the low oral bioavailability of doxorubicin
Ji-Eon Kim (2013)
Multidrug resistance: Physiological principles and nanomedical solutions.
S. Kunjachan (2013)
See more
Semantic Scholar Logo Some data provided by SemanticScholar