A novel formulation of [6]-gingerol: Proliposomes with enhanced oral bioavailability and antitumor effect

作者:Wang, Qilong; Wei, Qiuyu; Yang, Qiuxuan; Cao, Xia; Li, Qiang; Shi, Feng; Tong, Shan Shan; Feng, Chunlai; Yu, Qingtong; Yu, Jiangnan*; Xu, Ximing*
来源:International Journal of Pharmaceutics, 2018, 535(1-2): 308-315.
DOI:10.1016/j.ijpharm.2017.11.006

摘要

[6]-Gingerol, one of the components of the rhizome of Ginger, has a variety of biological activities such as anticoagulant, antioxidative, antitumor, anti-inflammatory, antihypertensive, and so forth. However, as one of the homologous phenolic ketones, [6]-gingerol is insoluble in water which limits its applications. Herein, we prepared [6]-gingerol proliposomes through modified thin-film dispersion method, which was spherical or oval, and physicochemically stable with narrow size distribution. Surprisingly, in vitro release of [6]-gingerol loaded proliposome compared with the free [6]-gingerol was significantly higher and its oral bioavailability increased 5-fold in vivo. Intriguingly, its antitumor effect was enhanced in the liposome formulation. Thus, our prepared [6]-gingerol proliposome proved to be a novel formulation for [6]-gingerol, which significantly improved its antitumor effect.