Intestinal transporters: enhanced absorption through P-glycoprotein-related drug interactions.
BACKGROUND
There are many factors that can affect the absorption process of orally administered drugs. Intestinal transporters play an important role in drug absorption. These transporters are divided into two major classes: the solute carriers and the ATP-binding cassette (ABC) transporters. P-glycoprotein (P-gp), belonging to the ABC transporter superfamily, flushes out the substrate drugs from a cell, thus regulating the intestinal absorption of drugs.


METHODS
This review gives a brief overview of uptake and efflux transporters localized in the intestine. However, because P-gp has been identified as an important underlying mechanism of drug interactions in humans, the review is strongly focused on summarizing the currently available data on the impact of P-gp for absorption of drugs.


CONCLUSIONS
The concomitant use of P-gp substrates and inhibitors (preferably in a single nanocarrier formulation) could be an effective and safe way to improve the bioavailability of drugs. It seems the study of P-gp and modulating its activity may be an interesting therapeutic goal to be considered in future research.
Tabriz University of Medical Sciences, Liver and Gastrointestinal Diseases Research Center and Faculty of Pharmacy , Tabriz , Iran.
Parvin
P
Zakeri-Milani
Hadi
H
Valizadeh
D018435:ATP Binding Cassette Transporter, Subfamily B / Q000378:metabolism*; D018528:ATP-Binding Cassette Transporters / Q000378:metabolism; D000284:Administration, Oral; D001682:Biological Availability; D004347:Drug Interactions / Q000502:physiology*; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology*; D004364:Pharmaceutical Preparations / Q000378:metabolism*
D018435:ATP Binding Cassette Transporter, Subfamily B; D018528:ATP-Binding Cassette Transporters; D004364:Pharmaceutical Preparations
P-glycoprotein; drug interaction; inhibitor; intestinal absorption; transporter