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Development of sesamin-loaded solid dispersion with α-glycosylated stevia for improving physicochemical and nutraceutical properties

Sato, Hideyuki, Aoki, Asako, Tabata, Aiko, Kadota, Kazunori, Tozuka, Yuichi, Seto, Yoshiki, Onoue, Satomi
Journal of functional foods 2017 v.35 pp. 325-331
Stevia, animal models, bioavailability, functional foods, pharmacokinetics, protective effect, rats, solubilization, spray drying
The present study aimed to enhance the nutraceutical properties of sesamin (SES) by solid dispersion (SD) approach using α-glycosylated stevia (Stevia-G) as a carrier compound with solubilizing effect. The SD formulations were characterized in terms of physicochemical and pharmacokinetic properties. The skin protective effect was evaluated in a rat model of drug-induced photodermatosis. The SES-loaded SD with Stevia-G (SES/Stevia-G-SD) prepared with spray-drying were uniform and spherical with a diameter of about 3μm, and SES within the formulation was found to be an amorphous state, possibly leading to improved dissolution behavior of SES. SES/Stevia-G-SD provided 190-fold increase in the dissolution amount of SES compared with crystalline SES. The oral bioavailability of SES/Stevia-G-SD (20mg-SES/kg) was 30-fold higher than that of crystalline SES. Orally-dosed SES/Stevia-G-SD (20mg-SES/kg) protected rat skins from drug-induced photodermatosis. Based on these findings, the SES/Stevia-G-SD approach might be efficacious to enhance the nutraceutical potential of SES.