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.