高良姜素-PLGA纳米粒的处方优化及其表征  

Prescription optimization and characterization of Galangin-PLGA nanoparticles

作　　者：陈莹子 朱蓉 孙旭怡 吴鑫福 张钰 羊玉英 魏娜[1] 秦贞苗[1] CHEN Ying‑zi;ZHU Rong;SUN Xu‑yi;WU Xin‑fu;ZHANG Yu;YANG Yu‑ying;WEI Na;QIN Zhen‑miao(School of Pharmacy,Hainan Medical University,Haikou 571199,China;School of Pharmacy,Changsha Medical University,Changsha,410219,China)

机构地区：[1]海南医学院药学院,海南海口571199 [2]长沙医学院药学院,湖南长沙410219

出　　处：《海南医学院学报》2021年第11期809-813,819,共6页Journal of Hainan Medical University

基　　金：国家自然科学基金资助项目(81660649);2019年海南医学院大学生创新创业训练计划项目(X201911810073)。

摘　　要：目的:以生物可降解材料聚乳酸-羟基乙酸共聚物(PLGA)为载体材料制备高良姜素-PLGA纳米粒(GL-PLGA NPs),并优化其处方。方法:采用改良乳化-溶剂挥发法制备纳米粒,HPLC测定高良姜素的含量。以粒径和包封率为指标,采用单因素和正交试验法优选处方,并对优化后的GL-PLGA NPs从表观形态、粒径分布、zeta电位、包封率进行质量评价。结果:高良姜素-PLGA纳米粒的最优处方条件为:有机相和水相的体积比为1∶8,聚乙烯醇浓度为1.5%,PLGA浓度为1.0%,药物浓度为0.2%。在此条件下制备的GL-PLGA NPs平均粒径为(249.00±2.44)nm,多分散系数为0.059,zeta电位为-4.86 mV,包封率为75.3%。电镜结果显示纳米粒呈球形,粒径大小均一,分散性良好。结论:该制备方法简单、稳定,可以得到粒径适宜、包封率较高的高良姜素-PLGA纳米粒。Objective:To make Galangin-PLGA nanoparticles(GL-PLGA NPs)using the polylactic-coglycolic acid(PLGA,a kind of biodegradable material)as the carrier material and to optimize the formulation.Methods:Nanoparticles were prepared through modified emulsification-solvent evaporation method,and the content of galangin was determined by HPLC.With particle size and entrapment efficiency as the indexes,single factor and orthogonal test were used to optimize the formulation.The surface configuration,particle size distribution,zeta potential,and entrapment efficiency of the optimized GL-PLGA NPs were evaluated.Results:The optimal prescription conditions of GL-PLGA NPs were as follows:the volume ratio of organic phase to aqueous phase was 1∶8,the concentration of polyvinyl alcohol was 1.5%,the concentration of PLGA was 1.0%,and the drug concentration was 0.2%.Under these conditions,the average particle size of GL-PLGA NPs was(249.00±2.44)nm,polydispersity index was 0.059,zeta potential was-4.86 mV,and the entrapment efficiency was 75.3%.The results of electron microscopy showed that the nanoparticles had sphericity,uniform particle size,and good dispersion.Conclusion:The preparation method is simple and stable,and GL-PLGA NPs with suitable particle size and high entrapment efficiency can be obtained through this method.

关 键 词：高良姜素 聚乳酸-羟基乙酸共聚物 纳米粒 正交试验 

分 类 号：R259[医药卫生—中西医结合]