Pharmaceutical Surfactants Interact Differently with the Human Efflux Transporters ABCB1 and ABCC2

摘要

Food, gastric stability, and metabolic processes as well as elimination processes via human efflux transporters like ABCB1 and ABCC2 can limit the extent of the oral bioavailability of drugs. In this context the knowledge that not only the drug but also the pharmaceutical excipients, especially surfactants, of a formulation may interact with these transporters is gaining increasing attention. Therefore, the interaction of different surfactants with ABCB1 and ABCC2 was investigated using in vitro cell assays. This study showed that the tested surfactants interact selectively with ABCB1 and ABCC2. Cremophor? EL and vitamin E TPGS inhibit both transporters. Pluronic? PE 10300 and sucrose ester L-1695 strongly inhibit ABCB1 whereas inhibitory activity of cremophor? RH 40 is observed on ABCC2 only.