Intestinal efflux transporters and drug absorption

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.

Keywords::

• ABC efflux transporters
• Biopharmaceutics Classification System (BCS)
• Breast cancer resistance protein
• Multi-drug resistance-associated proteins
• Oral bioavailability
• P-Glycoprotein

Disclosure statement

The review article submitted has not been previously published or simultaneously submitted elsewhere for publication. The manuscript has been read and approved by two authors.

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