Preparation and optimization of a resveratrol solid dispersion to improve the physicochemical properties and oral bioavailability of resveratrol

Abstract

Abstract Although resveratrol (RES) possesses potentially attractive activities, it has poor oral bioavailability due to its poor solubility. Solid dispersion (SD) is an efficient strategy to address the restricted dissolution rate and poor bioavailability of compounds that have poor water solubility. In this study, resveratrol solid dispersion (RES-SD) was prepared with mixture carriers through the melt method and optimized by an orthogonal array experimental design. The physicochemical properties and oral absorption of RES-SD formulations in vivo were measured. Analyses indicated that RES was dispersed in the optimal RES-SD formulation in the form of amorphous molecularly dispersed particles; as a result, the optimal SD exhibited a more than 80-fold increase in solubility and the dissolution rate was significantly improved relative to RES. Furthermore, pharmacokinetic studies in mice indicated that the optimal RES-SD formulation exhibited significantly improved RES oral bioavailability. Based on these findings, RES–SD developed through melt method was suitable for industrial production and avoid solvent remained. Moreover, the RES-SD with PEG6000 and F68 appears to be a promising approach to enhance the dissolution, bioavailability of RES. Graphical Abstract