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Enhanced oral bioavailability of [6]-Gingerol-SMEDDS: Preparation, in vitro and in vivo evaluation

Journal 2016 · IF 3.973 · 发表于 2016 年 10 月 28 日
作者: Yang Xu,Qilong Wang,Yingshu Feng,Caleb Kesse Firempong,Yuan Zhu,Emmanuel Omari-Siaw,Yuanyuan Zheng,Zunqin Pu,Ximing Xu,Jiangnan Yu
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摘要

The purpose of this study was to develop a [6]-Gingerol-loaded self-microemulsifying drug delivery system ([6]-Gingerol-SMEDDS) for oral administration and enhanced bioavailability of the drug. The [6]-Gingerol-SMEDDS, consisting of oils (ethyl oleate), surfactant (Cremophor EL35) and co-surfactant (1,2-propanediol), showed an acceptable spherical nanoparticle with stable physicochemical properties such as the mean droplet size (73.06 ± 0.49 nm), zeta potential (−2.45 ± 0.41) and encapsulation efficiency (89.40 ± 1.11%). The in vitro release of [6]-Gingerol from the delivery system in the three different media (HCl, pH 1.2; Double distilled water, pH 7.0; phosphate buffer solution, pH 7.4) was significantly higher than in the free drug. The [6]-Gingerol-SMEDDS also exhibited prolonged plasma circulation which led to 6.58-fold increase in oral bioavailability compared with the free drug. These findings indicated that the developed [6]-Gingerol-SMEDDS could be a promising alternative in improving the solubility and oral bioavailability of [6]-Gingerol, as well as increasing its biological applications.

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