Solidified phospholipid-TPGS as an effective oral delivery system for improving the bioavailability of resveratrol

Abstract

Resveratrol (RES), a compound with a variety of pharmacological activities, is reported to be poorly soluble in water and has limited absorption in vivo. And so its application is limited. In this study, a solidified RES phospholipid (PL) complex solid dispersion, containing RES-PL complex (RPC) and Sylysia 350 (S350) together with D-a-tocopheryl polyethylene glycol succinate (Vitamin E TPGS, or simply TPGS) (RPC-SDT) was prepared by simple solvent evaporation. The RPC-SDT was characterized by DSC, PXRD, SEM and IR analysis. All the data obtained confirmed that RES in RPC-SDT was in an amorphous state. The dissolution profile in vitro proved that RPC-SDT was able to markedly improve the dissolution rate. Single-pass intestinal perfusion studies showed that RPC improved the absorption slightly while TPGS increased the absorption nearly 2-fold. Finally, a pharmacokinetic study of RES and RPC-SDT in rats was investigated when it was found that RPC-SDT exhibited a higher peak plasma concentration (2392.8 vs. 702.3 ng mL−1), and increased AUC0–8h (3606.5 vs. 2188.5 ng mL−1 h）when compared with the raw RES, suggesting improved drug bioavailability. All the results obtained demonstrated that RPC-SDT significantly improved the bioavailability of RES by increasing both the dissolution rate and absorption.