Enhanced Oral Bioavailability of Resveratrol by Using Neutralized Eudragit E Solid Dispersion Prepared via Spray Drying.

Eun-Sol Ha,In-Hwan Baek,Du Hyung Choi,Min-Soo Kim,Heejun Park

doi:10.3390/antiox10010090

Abstract

In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

Highlights

Trans-resveratrol is an antioxidant phytochemical obtained from grapes, berries, and peanuts
We demonstrated that the oral bioavailability of trans-resveratrol can be increased by improving the dissolution rate and supersaturation of trans-resveratrol in an in vitro dissolution test
Trans-resveratrol solid dispersion powders with Eudragit E/HCl, HPMC, HPC, PVP, or PVP VA64 were prepared via spray drying

Summary

Introduction

Trans-resveratrol is an antioxidant phytochemical obtained from grapes, berries, and peanuts. In an attempt to improve the oral bioavailability of trans-resveratrol, several different strategies such as cyclodextrin complexes, cocrystals, liposomes, composite nanoparticles, solid dispersions, solid lipid nanoparticles, microemulsions, self-microemulsifying drug delivery systems, polymeric micelles, nanosuspensions, and nanocrystals have been used [8,9,10,11,12,13,14,15,16,17,18]. Most of these previous attempts have added a large amount of surfactant to the formulation. The absorption is typically higher for the formulations that use a lot of surfactants

Methods

Results

Conclusion