Teruo Murakami1, Mikihisa Takano. 1. Hiroshima International University, Faculty of Pharmaceutical Sciences, Laboratory of Biopharmaceutics and Pharmacokinetics, 5-1-1 Hiro-koshingai, Kure, Hiroshima 737-0112, Japan. t-muraka@ps.hirokoku-u.ac.jp
Abstract
BACKGROUND: The intestinal epithelial membrane expresses ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp), multi-drug resistance-associated proteins (MRPs) and breast cancer resistance protein (BCRP), in addition to various solute carrier (SLC) transporters. These ABC transporters affect the oral bioavailability of their substrate drugs. OBJECTIVE: To review the contribution of ABC efflux transporters such as P-gp, MRP2, MRP3, and BCRP in the intestinal absorption of substrate drugs. METHODS: Discussion was made by focusing on the site-specific expression and function of these ABC transporters, and the solubility and permeability of their substrate compounds. RESULTS/ CONCLUSION: The increase in the solubility and permeability of orally administered drugs could be the key to escape barrier function of ABC transporters, especially P-gp.
BACKGROUND: The intestinal epithelial membrane expresses ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp), multi-drug resistance-associated proteins (MRPs) and breast cancer resistance protein (BCRP), in addition to various solute carrier (SLC) transporters. These ABC transporters affect the oral bioavailability of their substrate drugs. OBJECTIVE: To review the contribution of ABC efflux transporters such as P-gp, MRP2, MRP3, and BCRP in the intestinal absorption of substrate drugs. METHODS: Discussion was made by focusing on the site-specific expression and function of these ABC transporters, and the solubility and permeability of their substrate compounds. RESULTS/ CONCLUSION: The increase in the solubility and permeability of orally administered drugs could be the key to escape barrier function of ABC transporters, especially P-gp.
Authors: Sneha V Gupta; Ellen J Sass; Melanie E Davis; Ryan B Edwards; Gerard Lozanski; Nyla A Heerema; Amy Lehman; Xiaoli Zhang; David Jarjoura; John C Byrd; Li Pan; Kenneth K Chan; A Douglas Kinghorn; Mitch A Phelps; Michael R Grever; David M Lucas Journal: AAPS J Date: 2011-05-04 Impact factor: 4.009