葛根素聚乳酸-羟基乙酸共聚物纳米粒制备及质量评价  

Preparation and Quality Evaluation of Puerarin-PLGA Nanoparticles

作　　者：王璐璐 甘昌冉 韦馨琳 胡婧怡 朱蓉 秦贞苗[1] WANG Lu-lu;GAN Chang-ran;WEI Xin-lin;HU Jing-yi;ZHU Rong;QIN Zhen-miao(School of Pharmacy,Hainan Medical University,Hainan Haikou 571199,China)

机构地区：[1]海南医学院药学院,海南海口571199

出　　处：《广州化工》2022年第11期29-33,共5页GuangZhou Chemical Industry

基　　金：海南省自然科学基金项目(No:821RC581);2020年海南医学院大学生创新创业训练计划项目(No:X202011810023);2019年海南医学院大学生创新创业训练计划项目(No:X201911810073)。

摘　　要：以生物可降解材料乳酸-羟基乙酸共聚物[poly(lactic-co-glycolic acid),PLGA]为载体,采用改良乳化溶剂挥发法制备葛根素(Puerarin,Pue)纳米粒(Pue-PLGA NPs)。以粒径和包封率为指标,采用单因素和正交试验优化处方工艺条件,并对优化后的Pue-PLGA NPs进行表观形态、粒径分布、Zeta电位及包封率质量评价。结果得到Pue-PLGA NPs的最佳处方工艺条件为聚乙烯醇浓度为1%,PLGA浓度为4 mg·mL^(-1),药物浓度为0.8 mg·mL^(-1),有机相和水相的体积比为1:8,超声时间为20 min。按最优处方工艺条件制备的纳米粒平均粒径为(149.2±4.8)nm,PDI为0.111±0.05,Zeta电位为-(5.73±0.12)mV,包封率为(71.31±0.57)%。电镜结果显示微粒呈球型,大小及分布均匀,粒子间无明显黏连。优选的处方工艺制备的Pue-PLGA NPs粒径适宜、包封率较高、理化性质稳定。Puerarin-PLGA nanoparticles(Pue-PLGA NPs)was prepared by modified emulsification-solvent evaporation method with the biodegradable materials-poly[poly(lactic-co-glycolic acid),PLGA]used as carrier materials.With particle size and entrapment efficiency as the indexes,single factor and orthogonal test were used to optimize the prescription process conditions.The quality of the optimized Pue-PLGA NPs was evaluated from the surface configuration,particle size distribution,zetapotential and entrapment efficiency.The results showed that the optimal prescription process conditions of Pue-PLGA NPseye drops were as follows:the concentration of PVA was 1.0%,the concentration of PLGA was 4 mg·mL^(-1),the drug concentration was 0.8 mg·mL^(-1),the volume ratio of organic phase to aqueous phase was 1:8 and the ultrasonic time was 20 min.Under these conditions,the average particle size of GL-PLGA NPs was(149.2±4.8)nm,PDI was 0.111±0.05,zetapotential was-(5.73±0.12)mV,the entrapment efficiency was(71.31±0.57)%.The results of electron microscopy showed that the particlesare spherical,uniform in size and distribution,and there was no obvious adhesion between the particles.Pue-PLGA NPs prepared by the optimized prescription process had suitable particle size,high entrapment efficiency,stable physical and chemical properties and good sustained release properties.

关 键 词：葛根素 PLGA纳米粒 正交试验 超滤法 

分 类 号：R944[医药卫生—药剂学]