Diet/Nutrient Interactions with Drug Transporters

This chapter focuses on the interactions of diet/nutrients with drug transporters arising from in vitro and in vivo studies, with specific emphasis on several major efflux transporters and uptake transporters. Most in vivo interaction studies reported to date are focused primarily on the interactions between dietary supplements and P-glycoprotein (P-gp). Given the facts that multidrug resistance associated protein (MRP) and breast cancer resistance protein (BCRP), organic anion-transporting polypeptide (OATP), and organic anion transporter (OAT) are also essential in drug disposition, it is important to appreciate the potential PK interactions of diet/nutrients with these transporters. The concentrations of many flavonoids required to produce significant modulation on activities of these transporters appear to be, in general, within the micro-molar range, which is achievable in the intestine after intake of food and, especially, after ingestion of dietary supplements.