Page 25 - 南京医科大学自然版

第45卷第2期 南京医科大学学报（自然科学版）
2025年2月 Journal of Nanjing Medical University（Natural Sciences） ·165 ·

·基础研究·

羟基积雪草苷和依克多因脂质体的制备及其功效研究

韦 伟 ，宋文鹏 ，吕 宁 ，环 飞 ，张晓玲 1*
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南京医科大学公共卫生学院卫生检验与检疫学系，江苏省医药农药兽药安全性评价与研究中心，江苏 南京 211166
1 2
［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 mV，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。
［关键词］ 羟基积雪草苷；依克多因；脂质体；舒缓功效
［中图分类号］ S853.73；R283.6 ［文献标志码］ A ［文章编号］ 1007⁃4368（2025）02⁃165⁃09
doi：10.7655/NYDXBNSN240790

Preparation and efficacy study of liposomes of madecassoside and ectoin

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WEI Wei ，SONG Wenpeng ，LÜ Ning ，HUAN Fei ，ZHANG Xiaoling 1*
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1 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
［Abstract］ 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.

［基金项目］“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）
通信作者（Corresponding author），E⁃mail：huanfei@njmu.edu.cn（ORCID：0009⁃0003⁃5904⁃6513）；zhangxl3@njmu.edu.cn（ORCID：
∗
0000⁃0001⁃6015⁃7817）