透明质酸修饰的葛根素PEG-PLGA纳米粒的处方工艺优化及其体外评价

Formulationandprocess Optimization of Puerarin-loaded PEG-PLGA Nanoparticles Modified by Hyaluronic Acid and Its in Vitro Evaluation

目的以乳酸-羟基乙酸共聚物(PEG-PLGA)为载体,优化纳米沉淀法制备透明质酸修饰的葛根素PEG-PLGA纳米粒(HA/Pue-NPs),并对其体外性质进行初步评价。方法以PEG-PLGA为载体材料,透明质酸为表面修饰剂,采用纳米沉淀法制备了透明质酸修饰的HA/Pue-NPs;应用正交实验设计优化处方,对其体外性质进行表征;并采用体外释药行为评价透明质酸修饰HA/Pue-NPs。结果制备出的载药纳米粒外观呈球形,平均粒径、Zeta电位分别为(88.9±2.2)nm、(-21.9±0.54)mV,载药量及包封率分别为6.75%、78.52%。体外释药试验表明,载药纳米粒释药缓慢,24h的累计释放率为65.8%。结论透明质酸修饰的葛根素PEG-PLGA纳米粒粒径大小均一,体外性质良好且具有一定的缓释特性。

OBJECTIVE With PEG-PLGA as the carrier,and the preparation of hyaluronic acid modified kudzu root element PEG-PLGA nanoparticles by nanoprecipitation method,to optimize the preparation prescription,and preliminary evaluation of its properties in vitro.METHODS With PEG PLGA as the carrier,Hyaluronic acid as surface modification agent,preparation of hyaluronic acid modified kudzu root element PEG-PLGA HA/Pue-NPs by nanoprecipitation method:design and optimize the prescription by Orthogonal experimental,characterize its in vitro properties,examine the in vitro drug release behavior of HA/Pue-NPs.RESULTS Prepared drug-loading nanoparticles has the spherical appearance.The average particle size and Zeta potential are(88.9±2.2)nm、(-21.9± 0.54)mV respectively,drug loadings and the coating rate are 6.75%,78.52%.In vitro drug release test shows that the drug-loading nanoparticles release slowly,the accumulative release rate is 65.8%within 24 h.CONCLUSION The particle size of HA/Pue-NPs is consistent,good in vitro properties and certain slow-release characterized.