羟基积雪草苷和依克多因复合活性成分脂质体的制备及其功效研究
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南京医科大学公共卫生学院卫生检验学系

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Preparation and efficacy of liposomes of Madecassoside and Ectoin
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Department of Hygienic Analysis and Detection,School of Public Health,NJMU

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    摘要:

    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。并检测其透皮效果。方法:细胞实验确定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1.2%。粒径为166.53 nm,电位为-29.63 mV,PDI为0.2,24 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

    Abstract:

    Abstract:Objective: A soothing liposome emulsion was developed by selecting Madecassoside and Ectoin as the primary ingredients. The transdermal absorption of the emulsion was subsequently evaluated. Method: The optimal ratio of Madecassoside and Ectoin, capable of eliciting anti-inflammatory and barrier repair activities, was identified through cellular assays. The preparation of hydroxy Madecassoside-Ectoin liposomes was conducted utilizing thin film hydration; subsequent characterization involved the determination of particle size, dispersibility coefficient, and charge using the Malvern particle size analyzer.The morphology was observed under projective electron microscope.The contents of Madecassoside and Ectoin in solution were determined by high performance liquid chromatography. The encapsulation rate and drug loading were determined by dialysis method. The transdermal characteristics of the liposome emulsion were evaluated via the Franz diffusion cell method. Results: A mass ratio of 1:9 for Madecassoside to Ectoin demonstrated optimal anti-inflammatory and barrier repair capabilities. 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 Madecassoside in the liposomes was 51.33%, the drug loading capacity of Madecassoside was 0.35%, the encapsulation rate of Ectoin was 26.39% and the drug loading capacity of Ectoin was 1.2%. The particle size is 166.53 nm, the potential is -29.63 mV, and the PDI is 0.2.Over a 24 hour period, the solution demonstrated a lower cumulative permeability compared to the aqueous control, without exhibiting an abrupt release; instead, a sustained release effect was observed. Conclusion: The liposome emulsion prepared in this experiment has a high drug load and stable internal particle distribution, and can achieve slow-release effect on the skin surface and prolong the action time of the effective substance.

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  • 收稿日期:2024-07-29
  • 最后修改日期:2024-11-25
  • 录用日期:2025-02-20
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