星点设计-效应面法优化青藤碱聚乳酸-羟基乙酸纳米粒的制备工艺  

Optimization of Preparation of Sinomenine PLGA Nanoparticles by Central Composite Design-Response Surface Methodology

作　　者：王婴[1,2,3] 李木生[3] 吴瑞婵 陈蓓蕊 吴新荣[2] 

机构地区：[1]广州中医药大学,广东广州510405 [2]广州军区广州总医院药学部,广东广州510010 [3]广东药科大学,广东广州510006

出　　处：《中药新药与临床药理》2017年第2期232-237,共6页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：国家自然科学基金资助项目(81673608);广东省科技计划项目(2015A020211034;2014A020212685)

摘　　要：目的制备青藤碱聚乳酸-羟基乙酸共聚物[poly(1actide-co-glycolide acid),PLGA]纳米粒,并优化该处方及其制备工艺。方法采用纳米沉淀法制备纳米粒,以青藤碱和PLGA的质量比、有机相和水相的体积比、表面活性剂聚氧乙烯氢化蓖麻油(RH40)的浓度为考察因素,以包封率和载药量为指标,通过星点设计-效应面法优化处方及制备工艺,并对其进行验证。结果青藤碱PLGA纳米粒的最佳处方和工艺条件为:青藤碱与PLGA的质量比1.4∶10;有机相与水相的体积比为2.2∶10,表面活性剂RH40的浓度为0.7%。制备的纳米粒平均粒径为113 nm,平均包封率为81.53%,平均载药量为7.65%。结论星点设计-效应面法简便可行,适用于青藤碱聚乳酸-羟基乙酸纳米粒的制备工艺优化。Objective To prepare sinomenine PLGA[poly（lactide-co-glycolide acid）] nanoparticles and to optimize the prescription and preparation of sinomenine PLGA nanoparticles. Methods Nanoparticles were prepared by nanoprecipitation method. The influence factors included the mass ratio of sinomenine to PLGA,the volume ratio of organic phase to water phase,and the concentration of surface activator polyoxyl 40 hydrogenated castor oil RH40.The prescription and preparation were optimized by central composite design-response surface methodology with the entrapment efficiency and drug loading as the evaluation parameters,and the prescription was validated. Results The optimum prescription and process conditions were as follows：the mass ratio of sinomenine to PLGA was 1.4∶10,the ratio of organic phase to water phase was 2.2∶10,and the concentration of RH40 was 0.7 %. The average particle size of nanoparticles was 113 nm,the average entrapment efficiency was 81.53 %,and the average drug loading rate was7.65 %. Conclusion The central composite design-response surface methodology is simple and feasible for the optimization of the preparation of sinomenine PLGA nanoparticles.

关 键 词：青藤碱 聚乳酸-羟基乙酸共聚物纳米粒 纳米沉淀法 星点设计-效应面法 

分 类 号：R284.2[医药卫生—中药学]