羟基积雪草苷和依克多因脂质体的制备及其功效研究  

Preparation and efficacy study of liposomes of madecassoside and ectoin

作　　者：韦伟[1] 宋文鹏 吕宁 环飞 张晓玲[1] WEI Wei;SONG Wenpeng;LÜNing;HUAN Fei;ZHANG Xiaoling(Department of Hygienic Analysis and Detection;Safety Assessment and Research Center for Drug,Pesticide and Veterinary Drug of Jiangsu Province,School of Public Health,Nanjing Medical University,Nanjing 211166,China)

机构地区：[1]南京医科大学公共卫生学院卫生检验与检疫学系 [2]江苏省医药农药兽药安全性评价与研究中心,江苏南京211166

出　　处：《南京医科大学学报(自然科学版)》2025年第2期165-172,184,共9页Journal of Nanjing Medical University(Natural Sciences)

基　　金：“科技攀登工程”科研创新项目(JX103SYL202200321);农药登记毒理学试验方法(省大仪平台分析测试研究课题)(D20190022)。

摘　　要：目的:选择羟基积雪草苷和依克多因为原料,制备一种具有舒缓功效的脂质体乳剂,并评价其透皮效果。方法:细胞实验探究能产生抗炎活性和屏障修复活性的羟基积雪草苷和依克多因的最佳配比;薄膜分散法制备羟基积雪草苷-依克多因脂质体;马尔文粒径仪测定其粒径、分散系数及电位;透射电镜下观察其形态;高效液相色谱法测定溶液中羟基积雪草苷及依克多因含量;透析法测定包封率和载药量;Franz扩散池测定脂质体的透皮情况。结果:细胞实验确定了羟基积雪草苷和依克多因按照质量比1∶9配比,其抗炎活性和屏障修复活性最佳。药物在此配比下,再按照磷胆比5∶1、药脂比1∶10条件下制备得到脂质体,该脂质体羟基积雪草苷包封率为51.33%、羟基积雪草苷载药量0.35%、依克多因包封率26.39%、依克多因载药量1.20%;粒径为166.53 nm,电位为-29.63 m V,PDI为0.20,24 h内累积透过量低于水溶液,无明显突释效应,具有缓释效果。结论:本实验制备的脂质体质量佳,内部颗粒分布均一较为稳定,同时可以达到在皮肤表面的缓释效果,延长功效物质的作用时间。Objective:To prepare a soothing liposome emulsion using madecassoside(MC)and ectoin(EC)as the primary ingredients and to evaluate its transdermal absorption.Methods:The optimal ratio of MC and EC that produced anti⁃inflammatory and barrier repair activities was determined through cellular assays;MC⁃EC liposomes were prepared using the thin film hydration.The particle size,dispersibility coefficient,and Zeta potential were measured using a Malvern particle size analyzer.The morphology was observed under transmission electron microscope.The contents of MC and EC in the solution were determined by high⁃performance liquid chromatography.The encapsulation rate and drug loading capacity were determined by the dialysis method.The transdermal characteristics of the liposome emulsion were evaluated via the Franz diffusion cell method.Results:The cell experiments determined that the best anti⁃inflammatory and barrier⁃repairing activities were achieved with a MC to EC mass ratio of 1∶9.Under these parameters,the liposome preparation conditions were optimized with a phosphorus⁃bile ratio of 5∶1 and a drug⁃to⁃lipid ratio of 1∶10.The encapsulation rate of MC in the liposomes was 51.33%,and the drug loading capacity of MC was 0.35%,the encapsulation rate of EC was 26.39%,and the drug loading capacity of EC was 1.20%.The liposomes had a particle size of 166.53 nm,the Zeta potential of-29.63 mV,and the PDI of 0.20.Over a 24 h period,the solution demonstrated a lower cumulative permeability compared with the aqueous control,without exhibiting an abrupt release;instead,a sustained release effect was observed.Conclusion:The MC and EC liposome emulsion prepared in this experiment has a high drug load and stable internal particle distribution,and may achieve slow⁃release effect on the skin surface and prolong the action time of the effective substance.

关 键 词：羟基积雪草苷 依克多因 脂质体 舒缓功效 

分 类 号：S853.73[农业科学—临床兽医学] R283.6[农业科学—兽医学]