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

• Main Authors: Hideyuki Sato, Asako Aoki, Aiko Tabata, Kazunori Kadota, Yuichi Tozuka, Yoshiki Seto, Satomi Onoue
• Format: Article
• Language: English
• Published: Elsevier 2017-08-01
• Series: Journal of Functional Foods
• Subjects: Oral absorption; Sesamin; Solid dispersion; Transglycosylated compounds; Drug-induced photodermatosis
• Online Access: http://www.sciencedirect.com/science/article/pii/S1756464617303092
• ISSN: 1756-4646

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 3 μm, 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 (20 mg-SES/kg) was 30-fold higher than that of crystalline SES. Orally-dosed SES/Stevia-G-SD (20 mg-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.