Improved oral absorption of (−)-epigallocatechin-3-gallate via self-double-emulsifying solid formulation

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• 作者：Caibiao Hu ; Qiang Wang ; Guodong Zhao ; Wenbing Yao and Qiang Xia
• 刊名：European Journal of Lipid Science and Technology
• 出版年：2016
• 出版时间：August 2016
• 年：2016
• 卷：118
• 期：8
• 页码：1115-1124
• 全文大小：551K
• ISSN：1438-9312

文摘

(−)-Epigallocatechin-3-gallate (EGCG), the main active ingredient from the green tea leaves (Camelia sinensis L.), is a hydrophilic drug with low-oral bioavailability (BCS class III). A novel self-double-emulsifying drug delivery system (SDEDDS) in solid form was formulated to improve the oral absorption of EGCG. Solubility of EGCG was determined in various components including water, oils, and surfactants. Pseudo-ternary phase diagrams were constructed to identify the most efficient self-emulsification region. The EGCG-SDEDDS in solid formulation rapidly formed fine water-in-oil-in-water emulsion. Furthermore, in vitro cellular experiments have shown increase in the cellular uptake of EGCG incorporated in SDEDDS compared to pure drug, and in an in vivo pharmacokinetic study in rats, the SDEDDS formulation exhibited 1.93-fold greater area-under-curve value than that of the drug solution. Stability studies have shown that solid EGCG-SDEDDS was stable up to 6 months under intermediate condition. These studies demonstrated that the novel SDEDDS in solid form could be a promising formulation strategy for the drug delivery of hydrophilic compounds with low-oral bioavailability.