丁香苦苷-PLGA纳米粒制备工艺的优选  

Optimizing the Formulation and Preparation Conditions of Syringopicroside Loaded PLGA Nanoparticles

作　　者：李梦雪[1] 吕邵娃[1] 杨志欣[1] 王艳宏[1] 李永吉[1] 

机构地区：[1]黑龙江中医药大学药学院,黑龙江哈尔滨150040

出　　处：《中医药学报》2012年第6期40-43,共4页Acta Chinese Medicine and Pharmacology

基　　金：高等学校博士学科点专项博导类科研基金资助项目(No.201123270009)

摘　　要：目的:以丁香苦苷(SYR)为模型药物,乳酸/羟乙酸共聚物(PLGA)为载体,优化纳米粒的制备工艺。方法:以W/O/W复乳化-溶剂挥发法制备SYR-PLGA纳米粒,采用正交试验设计优化处方组成和制备工艺,对纳米粒的外观形态、粒径、包封率和载药量等理化性质进行了检测。结果:优化后的工艺条件是SYR用量为10mg/mL、PLGA用量为20mg/mL、poloxamer188浓度为l%、二氯甲烷和乙酸乙酯组成的有机相比例为1∶3,SYR-PLGA纳米粒在透射电镜观察下的形态为类圆球形实体粒子,粒度分布较均匀,平均粒径为(133.4±0.97)nm,载药量为(6.01±0.21)%,包封率为(61.1±1.21)%。结论:该制备工艺简单、稳定。可以得到包封率和载药量较高、粒径适宜的丁香苦苷PLGA纳米粒。Objective： To prepare syringopicroside（SYR） loaded PLGA Nanoparticles and to study the release behavior of the nanoparticles in vitro.To optimize the preparation technique for nanoparticles by using SYR as model medicine and PLGA as controlled-release carrier.Methods： SYR loaded PLGA Nanoparticles were prepared by an w/o/w emulsion-solvent evaporation method.The formulation and the preparation conditions were optimized by orthogonal experiments using entrapment efficiency and medicine loading as the composite evaluation index.The Nanoparticles were evaluated by transmission electron microscope.The particle size distribution was evaluated by Mastersizer.The entrapment efficiency and the medicine loading were assessed.Results： The optimized parameters were SYR of 10mg/mL,PLGA of 20mg/mL,1%poloxamer188,Methylene chloride and ethyl acetate organic phase of ratio of 1：3.The results showed that SYR loaded PLGA nanoparticles were concinnous and spherical in shape.The mean diameter was（133.4±0.97）nm.The average entrapment efficiency was（61.1±1.21）% and medicine loading was（6.01±0.21）%.Conclusion：SYR loaded PLGA nanoparticles with a highly encapsulation efficiency,medicine loading,uniform size distribution are prepared by emulsion-solvent evaporation method.

关 键 词：丁香苦苷 聚乳酸 羟基乙酸共聚物 纳米粒 正交实验设计 

分 类 号：R284.1[医药卫生—中药学]