冰片修饰多柔比星/丹参酮ⅡA磺酸钠双载药纳米粒的制备及其理化性质
Preparation and characterization of doxorubicin-sodium tanshinoneⅡA sulfonate-loaded modifying borneol cationic nanoparticles
叶晓莉 1王丛瑶 2何佳 3庄建建 1尚小广 4林能明1
作者信息
- 1. 杭州市第一人民医院药学部,杭州 310006
- 2. 杭州市萧山区第一人民医院药剂科,杭州 311200
- 3. 树兰(杭州)医院护理部,杭州 310000
- 4. 杭州师范大学药学院,杭州 311121
- 折叠
摘要
目的 制备具有脑靶向的冰片(BO)修饰多柔比星(DOX)/丹参酮ⅡA磺酸钠(STS)双载药纳米粒(BO-DOX/STS-NPs)并对其理化性质进行考察.方法 采用复乳溶剂挥发法制备BO-DOX/STS-NPs,正交设计后以包封率和载药量为评价指标优化处方工艺.结果 制备BO-DOX/STS-NPs的优化条件:药物与PEG2000-PLA的质量比为1∶20,外水相PVA的体积浓度为3%,内水相与有机相体积比为1∶10,有机相与外水相体积比为1∶10.按优化条件所制备的BO-DOX/STS-NPs粒径为(114.75±1.39)nm,Zeta 电位为(-6.58±0.02)mV,DOX 与 STS 的包封率分别为(97.34±0.97)%和(98.21±0.73)%,载药量分别为(2.40±0.03)%和(1.18±0.01)%,药物释放曲线均符合Ritger-Peppas方程模型.结论 采用复乳溶剂挥发法成功制备了 BO-DOX/STS-NPs,确定了最优制备处方和制备工艺.所制备的纳米粒粒径分布均一、稳定性好、载药量高,具有缓释效果.
Abstract
AIM To prepare Doxorubicin-Sodium tanshinone Ⅱ A sulfonate-loaded modifying borneol cationic nanoparticles(BO-DOX/STS-NPs)with brain targeting property.METHODS The BO-DOX/STS-NPs were prepared with the double emulsion solvent evaporation method and were optimized through the orthogonal test according to entrapped efficiency and drug loading of BO-DOX/STS-NPs.RESULTS The optimal conditions for preparation of BO-DOX/STS-NPs were as follows:the mass ratio of drug to PEG2000-PLA was 1∶20,the volume concentration of PVA in the external aqueous phase was 3%,the volume ratio of internal water phase to oil phase was 1∶10,and the volume ratio of oil phase to outer water phase was 1∶10.The mean particle size of the resulted BO-DOX/STS-NPs was(114.75±1.39)nm and Zeta potential was(-6.58±0.02)mV.The average entrapped efficiency was(97.34±0.97)%for DOX and(98.21±0.73)%for STS.The drug-loading capacity was(2.40±0.03)%for DOX and(1.18±0.01)%for STS.The drug release curves for both drugs conformed to the Ritger-Peppas equation model.CONCLUSION An optimized nanoparticle drug delivery system is obtained by the double emulsion method.The optimized nanoparticles have uniform particle size distribution,good stability,high drug loading and sustained release effect.
关键词
多柔比星/丹参酮ⅡA磺酸钠/冰片/纳米粒/正交设计Key words
doxorubicin/sodium tanshinone ⅡA sulfonate/borneol/nanoparticle/orthogonal design引用本文复制引用
基金项目
杭州市医学重点学科建设项目(杭卫发[2021]21号)
浙江省医学重点学科建设项目(浙卫办[2018]2号)
浙江省临床肿瘤药理与毒理学研究重点实验室项目(2020E10021)
浙江省中医药科技计划(2014ZA083)
浙江省中医药科技计划(2021ZA111)
浙江省卫生健康科技计划(2021KY865)
杭州市卫生科技计划(A20210186)
浙江省药学会医院药学专项科研基金(2020ZYY28)
出版年
2024