Enhanced pharmacokinetic behavior and hepatoprotective function of ginger extract-loaded supersaturable self-emulsifying drug delivery systems. (January 2018)

• Record Type: Journal Article
• Authors: Ogino, Mizuki; Yakushiji, Keisuke; Suzuki, Hiroki; Shiokawa, Kenichi; Kikuchi, Hiroshi; Seto, Yoshiki; Sato, Hideyuki; Onoue, Satomi
• Is Part Of: Journal of functional foods. Volume 40(2018)
• Page Start: 156
• Page End: 163
• Publication Date: 2018-01
• Subjects: ALT alanine aminotransferase -- ANOVA analysis of variance -- CCl4 carbon tetrachloride -- COX-2 cyclooxygenase-2 -- DLS dynamic light scattering -- ESI electrospray ionization -- GI gastrointestinal -- 6G 6-gingerol -- 8G 8-gingerol -- GE ginger extract -- HPMC hydroxypropyl methyl cellulose -- MCT medium-chain triglyceride -- SEDDS self-emulsifying drug delivery systems -- 6S 6-shogaol -- SCF supercritical fluid -- S-SEDDS supersaturable self-emulsifying drug delivery systems -- TEM transmission microscopy -- UPLC ultra-performance liquid chromatography; Ginger extract -- Hepatoprotective function -- Oral absorption -- Supersaturable self-emulsifying drug delivery systems; Functional foods -- Analysis -- Periodicals; Food -- Biotechnology -- Periodicals; Nutrition -- Periodicals; 613.2
• DOI: 10.1016/j.jff.2017.08.035
• Languages: English
• ISSNs: 1756-4646

Abstract

Highlights: Novel solubilizing system for ginger extract (GE) was successfully developed. Dissolution behavior of GE was significantly enhanced by emulsification. GE-loaded formulation improved oral absorption of active ingredients in GE. Orally-dosed GE formulation could inhibit CCl4 -induced hepatotoxic injury in rats. Abstract: The aim of present study was to enhance the nutraceutical properties of ginger extract (GE) by employing supersaturable self-emulsifying drug delivery systems (S-SEDDS). SEDDS of GE (SEDDS/GE), consisting of medium-chain triglyceride, lysolecithin and glycerin, was produced. To prepare S-SEDDS of GE (S-SEDDS/GE), hydroxypropyl methylcellulose was added to the SEDDS/GE as a precipitation inhibitor. Physicochemical, pharmacokinetic, and hepatoprotective properties of GE formulations were characterized. Both formulations improved the dissolution behavior of GE due to the formation of fine micelles with a median diameter of ca. 110 nm. After oral administration of GE samples in rats, the relative bioavailabilities of 6-gingerol and 8-gingerol in the S-SEDDS/GE-treated group were ca. 3-fold higher than those of GE-treated group, respectively. Repeated oral administration of GE/S-SEDDS (100 mg-GE/kg) provided a hepatoprotective effect in a rat model of carbon tetrachloride-induced hepatotoxicity. From these observations, the S-SEDDS approach might be efficacious for enhancing the nutraceutical properties of GE.