| Summary: | The aim of this study was to prepare pure <i>trans</i>-resveratrol nanoparticles without additives (surfactants, polymers, and sugars) using a supercritical antisolvent (SAS) process with alcohol (methanol or ethanol) and dichloromethane mixtures. In addition, in order to investigate the effect of particle size on the dissolution and oral bioavailability of the <i>trans</i>-resveratrol, two microparticles with different sizes (1.94 μm and 18.75 μm) were prepared using two different milling processes, and compared to <i>trans</i>-resveratrol nanoparticles prepared by the SAS process. The solid-state properties of pure <i>trans</i>-resveratrol particles were characterized. By increasing the percentage of dichloromethane in the solvent mixtures, the mean particle size of <i>trans</i>-resveratrol was decreased, whereas its specific surface area was increased. The particle size could thus be controlled by solvent composition. <i>Trans</i>-resveratrol nanoparticle with a mean particle size of 0.17 μm was prepared by the SAS process using the ethanol/dichloromethane mixture at a ratio of 25/75 (<i>w</i>/<i>w</i>). The in vitro dissolution rate of <i>trans</i>-resveratrol in fasted state-simulated gastric fluid was significantly improved by the reduction of particle size, resulting in enhanced oral bioavailability in rats. The absolute bioavailability of <i>trans</i>-resveratrol nanoparticles was 25.2%. The maximum plasma concentration values were well correlated with the in vitro dissolution rate. These findings clearly indicate that the oral bioavailability of <i>trans</i>-resveratrol can be enhanced by preparing pure <i>trans</i>-resveratrol nanoparticles without additives (surfactants, polymers, and sugars) by the SAS process. These pure <i>trans</i>-resveratrol nanoparticles can be applied as an active ingredient for the development of health supplements, pharmaceutical products, and cosmetic products.
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