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Updated: Jun 25, 2026

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
Published on: October 18, 2013
Intestinal efflux transporters and drug absorption
Teruo Murakami1, Mikihisa Takano
1Hiroshima 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
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.
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