星点设计-效应面法优化mPEG-PLGA嵌段共聚物空白纳米粒的制备工艺  

Optimization of Preparation Process of mPEG-PLGA Block Copolymer Blank Nanoparticles by Central Point Design-response Surface Method

作　　者：张卫敏[1] 贾莉[1] 赵鲁亚[1] 李丽平[1] 李伟男[2] ZHANG Weimin;JIA Li;ZHAO Luya;LI Liping;LI Weinan(Heze Medical College,Heze Shandong 274000,China;Heilongjiang University of Traditional Chinese Medicine,HarbinHeilongjiang 150040,China.)

机构地区：[1]菏泽医学专科学校,山东菏泽274000 [2]黑龙江中医药大学,黑龙江哈尔滨150040

出　　处：《药品评价》2022年第24期1480-1484,共5页Drug Evaluation

基　　金：山东省中医药科技项目(2021M204)。

摘　　要：目的:优化乳化挥发法制备的聚乙二醇-聚乳酸-羟基乙酸(mPEG-PLGA)嵌段共聚物空白纳米粒制备工艺。方法:采用单因素影响因素实验,以粒径和多分散系数为评价指标,考察共聚物种类和浓度、乳化剂的种类和浓度、油水两相比例,搅拌速率和离心方式等不同影响因素,初步确定制备空白纳米粒的最佳条件。结合星点设计-效应面法(CCD-RSM)确定空白纳米粒的最优处方,并对最优处方进行工艺验证。结果:采用10.41 mg/mL的共聚物浓度、1∶2的油水两相比例、0.21%的乳化剂浓度、870 rpm的磁力搅拌速率,制备的空白纳米粒粒径为(90.74±2.9)nm、多分散系数为0.22±0.08。结论:以最优处方和工艺制备的空白纳米粒粒径和多分散系数均较小,该处方及工艺可行。Objective:To optimize the preparation process of polyethylene glycol-polylactic acid-hydroxyacetic acid(mPEGPLGA)block copolymer blank nanoparticles prepared by emulsification and volatilization.Methods:Single factor experiment was preliminary carried out to determine the optimum conditions for the preparation of blank nanoparticles by investigating different influencing factors,such as copolymer type and concentration,emulsifier type and concentration,oil-water phase ratio,stirring rate and centrifugation method,using particle size and polydispersion index as evaluation indexes.Combined with central point design-response surface method(CCD-RSM),the optimal formulation of blank nanoparticles was determined,and the optimal formulation was validated.Results:Using the copolymer concentration of 10.41 mg/mL,oil-water phase ratio of 1∶2,emulsifier concentration of 0.21%,magnetic stirring rate of 870 rpm,the size of blank nanoparticles was 90.74±2.9 nm,and the polydispersion index was 0.22±0.08.Conclusion:The blank nanoparticles prepared by the optimal formulation and process have smaller particle size and polydispersion index,and the formulation and process are feasible.

关 键 词：工艺学 制药 mPEG-PLGA嵌段共聚物 纳米粒 挥发法 星点设计-效应面法 

分 类 号：R943[医药卫生—药剂学]