生物等效性和生物利用度杂志

抽象的

The Potential of Non-Ionic Surfactant Against P-Glycoprotein Efflux Transporters for Drug Development System

Kulsirirat T, Rukthong P, Dechwongya P and Sathirakul K

Polysorbates (Tweens) are widely used in pharmaceutical formulations as excipients, such as stabilizer or solubilizer, for poorly soluble drugs. The efflux transporters ABCB1 (P-glycoprotein, P-gp) play an essential role in limiting the oral bioavailability of drugs. P-gp is expressed in the intestinal epithelium, thereby, it significantly impairs the systemic absorption of various active substances. The present study is to investigate a new property of polysorbates including its ability to stimulate or inhibit the efflux transporter P-glycoprotein (P-gp) using Pgp-Glo™ assay systems. The Pgp-GloTM assay systems are luminescent P-glycoprotein (P-gp) ATPase assays. It detected the effect of substance on recombinant human P-gp in a cell membrane fraction. The investigation showed that the concentration of 0.1% Tween 80 is an inhibitor of P-gp ATPase activity, whereas, the concentrations of 0.5% and 1% of Tween 80 demonstrated as a stimulator. All of these concentrations of Tween 20 were observed to be an inhibitory effect on P-gp ATPase activity.