透明质酸修饰的阿奇霉素/槲皮素胶束处方优选及体外靶向性考察
Formulation Optimization and in vitro Targeting of Hyaluronic Acid-modified Azithromycin/Quercetin Micelles
张子湑 1王佳华 1刘茉 1陈沐含 1于洋 1孔亮 1李学涛1
作者信息
- 1. 辽宁中医药大学 药学院,辽宁 大连 116600
- 折叠
摘要
目的 优化透明质酸修饰的阿奇霉素/槲皮素胶束的处方,研究RAW264.7细胞的主动靶向性.方法 采用薄膜分散法制备透明质酸修饰的阿奇霉素/槲皮素胶束,利用Box-Benhken响应面法对影响其包封率的三因素[聚乙烯己内酰胺-聚乙酸乙烯酯聚乙二醇接枝共聚物(Soluplus)和槲皮素(Qe)质量比、Soluplus和聚乙二醇1000维生素E琥珀酸酯(TPGS1000)质量比、水化温度]进行优化,并验证胶束的包封率.通过荧光显微镜和流式细胞仪来考察胶束对RAW264.7细胞的主动靶向性.结果 确定最优处方为Soluplus:Qe=30:1,Soluplus:TPGS1000=4:1,水化温度为40 ℃.经实验验证,透明质酸修饰的阿奇霉素/槲皮素胶束中阿奇霉素和槲皮素两药的平均包封率为(90.55±1.25)％.不同组胶束中阿奇霉素浓度为0.312 5～20µM范围内对RAW264.7细胞活力无影响.体外靶向性实验结果表明经透明质酸修饰后的胶束对RAW264.7细胞的靶向性增强.结论 最优处方制备的胶束具有较高的包封率,经透明质酸修饰的胶束对RAW264.7细胞具有良好的靶向性.
Abstract
Objective To optimize the formulation of hyaluronic acid-modified azithromycin/quercetin micelles and evaluate the active targeting of RAW264.7 cells.Methods The HA modified azithromycin/quercetin micelles were prepared by thin film dispersion method.The Box-Benhken response surface method was used to optimize the three factors affecting the encapsulation efficiency of the micelles(mass ratio of soluplus to quercetin,mass ratio of soluplus to TPGS1000,and hydration temperature),and the encapsulation efficiency of the micelles was verified.The active targeting of the micelles to RAW264.7 cells was examined by fluorescence microscopy and flow cytometry.Results The optimal prescription was determined as Soluplus:Qe=30:1,Soluplus:TPGS=4:1,and the hydration temperature was 40℃.The average encapsulation efficiency of azithromycin and quercetin in hyaluronic acid-modified azithromycin/quercetin micelles was(90.55±1.25)％.The micelle of different groups had no effect on the viability of RAW264.7 cells when the concentration of azithromycin ranged from 0.312 5 to 20 μM.In vitro targeting experiments showed that the HA modified micelles had enhanced targeting ability to RAW264.7 cells.Conclusion The optimal formulation of the micelles has a high encapsulation efficiency,and the HA modified micelles have a good targeting ability to RAW264.7 cells.
关键词
阿奇霉素/槲皮素/透明质酸/胶束/处方优选/靶向性Key words
Azithromycin/quercetin/hyaluronic acid/micelles/prescription optimization/active targeting引用本文复制引用
出版年
2024
NETL
NSTL
万方数据