白藜芦醇柔性脂质体的制备及其体外评价  

Preparation and in vitro evaluation of resveratrol elastic liposomes

作　　者：钟玮 王俊 张玉洁 王中彦[2] ZHONG Wei;WANG Jun;ZHANG Yu-jie;WANG Zhong-yan(School of Traditional Chinese Medica,Shenyang Pharmaceutical University,Shenyang 110016,China;School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学中药学院,沈阳110016 [2]沈阳药科大学药学院,沈阳110016

出　　处：《中国新药杂志》2024年第2期187-193,共7页Chinese Journal of New Drugs

摘　　要：目的:制备白藜芦醇柔性脂质体,并考察其体外特性.方法:采用乙醇注入法制备脂质体,以包封率、粒径为指标,通过单因素考察和星点设计-响应面法优化白藜芦醇脂质体处方;以皮肤滞留量筛选表面活性剂的配比,制备白藜芦醇柔性脂质体;并对其表面特征、粒径、Zeta电位、体外释放度及皮肤滞留进行考察.结果:最终处方:大豆卵磷脂量为7.5mg·mL-1,磷脂-胆固醇的质量比为3.16∶1,磷脂-白藜芦醇的质量比为30.28∶1,磷脂-吐温-80的质量比为3∶1.制得的白藜芦醇柔性脂质体的平均粒径为(143.70±1.74)nm,多分散系数(PDI)为(0.092±0.060),Zeta电位为-(9.65±0.61)mV.体外释放研究表明,白藜芦醇乙醇溶液在4h释放了80%,达到释放平衡;白藜芦醇柔性脂质体在8h时的累计释放度为54%,24h内持续缓慢释放,符合Higuchi动力学模型.皮肤滞留实验结果表明,其在2~6h时皮肤滞留量缓慢升高,证明其可以缓慢释放,且在6h时达到34.14μg·cm-2.结论:优选的柔性脂质体重现性好、包封率高、粒径小,具有明显的缓释效果,皮肤滞留量高,适合于局部给药.Objective:To prepare resveratrol elastic liposomes and investigate their in vitro properties.Methods:Liposomes were prepared by ethanol injection method.The formulation of resveratrol liposomes was optimized by single factor investigation and central composite design-response surface methodology with encapsulation efficiency and particle size as indexes.The ratio of surfactants was screened by skin retention;the surface characteristics,particle size,Zeta potential,in vitro release,and skin retention were determined.Results:The final prescription was as follows:the amount of soybean lecithin was7.5mg·mL-1,the mass ratio of phospholipid to cholesterol was 3.16∶1,the mass ratio of phospholipid to resveratrol was 30.28∶1,and the mass ratio of phospholipid to Tween-80 was3∶1.The average particle size of the prepared resveratrol elastic liposomes was(143.70±1.74)nm,the polydispersity index(PDI)was(0.092±0.060),and the Zeta potential was-(9.65±0.61)mV.In vitro release studies showed that resveratrol ethanol solution released 80%at 4 h,reaching release equilibrium.The cumulative release of resveratrol elastic liposomes at 8 h was 54%,and the release of resveratrol elastic liposomes continued slowly within 24 h,which was consistent with the Higuchi kinetic model.The results of skin retention test showed that its skin retention increased slowly at 2~6 h,proving that it could release slowly and reached 34.14μg·cm-2 at 6 h.Conclusion:The optimized elastic liposomes had good reproducibility,high encapsulation rate and small particle size,obvious sustained release effect and high skin retention.

关 键 词：白藜芦醇 柔性脂质体 体外释放 离体经皮渗透试验 滞留量 

分 类 号：R943[医药卫生—药剂学]