Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.
Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.
Int J Pharm. 2018 Jan 15;535(1-2):308-315. doi: 10.1016/j.ijpharm.2017.11.006. Epub 2017 Nov 7.
[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.
[6]-姜烯酚是姜根茎的成分之一，具有多种生物活性，如抗凝、抗氧化、抗肿瘤、抗炎、降压等。然而，作为同源酚酮之一，[6]-姜烯酚不溶于水，这限制了它的应用。本文通过改良薄膜分散法制备了[6]-姜烯酚前体脂质体，其为球形或椭圆形，理化性质稳定，粒径分布较窄。令人惊讶的是，与游离[6]-姜烯酚相比，[6]-姜烯酚包封于前体脂质体中的体外释放明显增加，体内生物利用度增加了 5 倍。有趣的是，其在脂质体配方中的抗肿瘤效果增强。因此，我们制备的[6]-姜烯酚前体脂质体被证明是[6]-姜烯酚的一种新型制剂，显著提高了其抗肿瘤效果。
