Development of a Solid Dispersion System for Improving the Oral Bioavailability of Resveratrol in Rats

Background and Objective Resveratrol (3,4',5-trihydroxy-trans-stilbene; RES) produces a variety of pharmacological effects; however, its oral bioavailability (BA) approaches zero. In this study, grape peel extract (GPE) was incorporated into a solid dispersion delivery system to improve the solubility, dissolution and oral absorption of RES. Methods The dripping pill (DP) oral delivery system was developed through the hot-melt method, and the optimal formulation consisted of GPE, propylene glycol monocaprylate, poloxamer 188, polyoxyl 35 castor oil and polyethylene glycol 6000. Results The DPs enhanced the (mean +/- SD) dissolution of RES from 23.3 +/- 1.0 to 67.8 +/- 0.4 %. The pharmacokinetic profiles in the rats revealed that the DPs increased the oral BA of RES from 0.9 +/- 0.1 to 10.5 +/- 0.9 %; this represented an approximately 12-fold increase in absorption. Conclusions Our results indicated that the DP formulation improves the dissolution and oral BA of RES. Thus, this could be an effective and practical technique for food and pharmaceutical applications.