表没食子儿茶素没食子酸酯二元醇脂质体的制备及体外透皮性质研究

Study on the preparation and in vitro transdermal penetration of epigallocatechin-3-gallate binary ethosomes

目的制备表没食子儿茶素没食子酸酯二元醇脂质体(EGCG-EL),并对其体外透皮性质进行研究。方法采用乙醇注入法制备EGCG-EL,以激光粒度仪测定EGCG-EL的粒度及其分布和Zeta电位,超滤–HPLC法测定包封率,Franz扩散装置考察EGCG-EL的体外透皮特性。结果所制备的脂质体粒径分布均匀,平均粒径为(144.5±11.3)nm,PDI为0.19±0.04,Zeta电位为–34.8 mV。EGCG-EL的包封率达(65.91±1.45)%,体外透皮试验结果显示,与普通的EGCG溶液剂相比,EGCG-EL皮肤内药物的滞留量明显增加(P<0.001)。结论该制剂制备简便、质量稳定,是一种优良、安全的皮肤科外用制剂。

Objective To prepare the epigallocatechin-3-gallate binary ethosomes(EGCG-EL)and evaluate its in vitro percutaneous diffusion characteristics.Methods EGCG-EL was prepared by ethanol injection method.The particle size,zeta potential and encapsulation efficiency of EGCG-EL were measured by laser scattering particle size distribution analyzer and ultrafiltration–HPLC method.Franz diffusion cell was used to investigate percutaneous diffusion characteristics of the EGCG-EL in vitro.Results The EGCG-EL had an average size of(144.5±11.3)nm with PDI of 0.19±0.04.The surface charge of EGCG-EL was-34.8 mV.Moreover,EGCG was readily to be incorporated into ethosomes with encapsulation efficiency of(65.91±1.45)%.The results of the transdermal penetration study showed the retention amount of the EGCG-EL was significantly higher than that in EGCG solution(P<0.001).Conclusion The preparation technology for EGCG-EL is simple and stable,and the prepared EGCG-EL is a superior and safe new preparation for external application in dermatology.