降钙素/葛根素双载药纳米粒的制备及体外释药的研究  

Preparation and in Vitro Release of Chitosan-Calcitonin/Puterrin-Dual-Loaded PLGA Nanoparticles

作　　者：杨慧[1] 柳琳[2] 朱潇冉 钱丽梅[1] 张幸国[2] 

机构地区：[1]浙江中医药大学药学院,杭州310053 [2]浙江大学医学院附属第一医院药剂科,杭州310003

出　　处：《中国药学杂志》2016年第7期561-566,共6页Chinese Pharmaceutical Journal

基　　金：浙江省自然科学基金资助项目(LQ15H280004)

摘　　要：目的制备以壳聚糖(chitosan,CS)修饰的降钙素/葛根素聚乳酸-羟基乙酸共聚物双载药纳米粒(chitosan-calcitonin/puerarin-PLGA-dual-loaded nanoparticles,CS-CT/PR-NPs),并考察其理化性质及体外释药特性。方法以聚乳酸-羟基乙酸共聚物为载体材料,采用复乳溶剂蒸发法制备壳聚糖修饰的降钙素/葛根素聚乳酸-羟基乙酸共聚物双载药纳米粒;正交实验优化其处方工艺;透射电镜及激光粒度仪分别考察其形态、粒径和Zeta电位,高速离心法测定包封率及载药量双载药纳米粒;透析袋法考察其体外释药特性。结果制备的壳聚糖修饰的降钙素/葛根素聚乳酸-羟基乙酸共聚物双载药纳米粒外观呈椭圆形,平均粒径为(190±2.65)nm,多分散指数为(0.117±0.027),Zeta电位为(16.5±1.08)m V,降钙素的包封率和载药量分别为(75.7±1.15)%,(3.47±0.31)%,葛根素的包封率和载药量分别为(50.9±1.08)%,(4.68±0.19)%;体外释药具有缓释特征。结论本实验成功制备载有双药的壳聚糖修饰的降钙素/葛根素聚乳酸-羟基乙酸共聚物双载药纳米粒,2种药物的包封率均较高,体外释药均具有明显的缓释特征,为提高降钙素的口服生物利用度提供了可能,也为双载药纳米粒的制备提供实验参考。OBJECTIVE To prepare calcitonin / puerarin-PLGA-dual-loaded nanoparticles modified by chitosan,and investigate theirin vitro release behavior. METHODS CS-CT / PR-NPs were prepared by the double emulsion solvent evaporation technique with PLGA as a carrier material; the formulation of CS-CT / PR-NPs was optimized by orthogonal design; the morphology of CS-CT / PR-NPs was observed by transmission electron microscope; the mean particle size,particle size distribution and Zeta potential were measured by laser particle size analyzer; the entrapment efficiency and drug loading were measured by ultracentrifugation; the in vitro release behavior was studied by dialysis. RESULTS CS-CT / PR-NPs were spherical in shape with the mean particle size of（ 190 ± 2. 65） nm,particle size distribution of（ 0. 117 ± 0. 027） and Zeta potentialof（ 16. 5 ± 1. 08） m V. The entrapment efficiency was（ 75. 7 ± 1. 15） %,and the drug loading of CT was（ 3. 47 ± 0. 31） %,while those of PR were（ 50. 9 ± 1. 08） % and（ 4. 68 ± 0. 19） %,respectively. The profiles of in vitro release had the features of sustained-release. CONCLUSION CS-CT / PR-NPs are prepared successfully and show a sustained-release characteristic with high entrapment efficiency,which may improve the oral bioavailability of CT and provide the experimental reference for preparing the dual-loaded nanoparticles.

关 键 词：降钙素 葛根素 聚乳酸-羟基乙酸共聚物 双载药纳米粒 体外释药 

分 类 号：R944[医药卫生—药剂学]