Development of sesamin-loaded solid dispersion with α-glycosylated stevia for improving physicochemical and nutraceutical properties. (August 2017)

• Record Type: Journal Article
• Authors: Sato, Hideyuki; Aoki, Asako; Tabata, Aiko; Kadota, Kazunori; Tozuka, Yuichi; Seto, Yoshiki; Onoue, Satomi
• Is Part Of: Journal of functional foods. Volume 35(2017)
• Page Start: 325
• Page End: 331
• Publication Date: 2017-08
• Subjects: ANOVA one-way analysis of variance -- DSC differential scanning calorimetry -- ESI electric spray ionization -- Hesperidin-G α-glycosylated hesperidin -- PLM polarized light microscopy -- RH relative humidity -- Rutin-G α-glycosylated rutin -- SD solid dispersion -- SEM scanning electron microscopy -- SES sesamin -- Stevia-G α-glycosylated stevia -- TF trifluoperazine -- UPLC ultra performance liquid chromatography -- UV ultra violet -- PXRD X-ray powder diffraction; Oral absorption -- Sesamin -- Solid dispersion -- Transglycosylated compounds -- Drug-induced photodermatosis; Functional foods -- Analysis -- Periodicals; Food -- Biotechnology -- Periodicals; Nutrition -- Periodicals; 613.2
• DOI: 10.1016/j.jff.2017.05.054
• Languages: English
• ISSNs: 1756-4646

Abstract

Highlights: Alpha-glycosylated stevia improved the aqueous solubility of sesamin (SES). SES-loaded solid dispersion (SD) system markedly enhanced oral absorption of SES. Orally-dosed SES-loaded SD suppressed drug-induced photodermatosis in rats. Novel SD system might be promising to enhance the nutraceutical potential of SES. Abstract: 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.