抗癫疒间肽纳米粒的制备及体外释药性能的研究

Preparation of anti-epilepsy peptide nanoparticles and investigation of the drug releasing characteristic in vitro

目的制备抗癫疒间肽纳米粒,并研究其体外释药性能。方法选用聚乙二醇-聚乳酸-聚乙醇酸嵌段共聚物为载体,采用复乳-溶剂挥发法制备抗癫疒间肽纳米粒,以包封率、载药量等指标优化制备工艺,并研究纳米粒体外释药性能。结果抗癫疒间肽纳米粒外观呈圆形或类圆形,平均粒径为(100.2±2.45)nm,包封率和载药量分别为(64.46±1.34)%和(4.73±0.32)%,体外释药呈现缓释和突释两个阶段,符合Weibull方程。结论建立的制备工艺简便可行,得到的抗癫疒间肽纳米粒包封率和载药量较高,粒径小,体外释药具有明显的缓释特征。

Objective To prepare anti-epilepsy peptide nanoparticles and evaluate its release characteristics in vitr. Methods Anti-epilepsy peptide nanoparticles were prepared by emulsion/solvent evaporation method and poly （ethylene glycol）-poly（lactide acid）-poly（glycolic acid）copolymer was used as carrier material. Encapsulation effi-ciency and drug loading were used to optimize the technique and evaluate its release characteristics in vitro. Results The appearance of all anti-epilepsy peptide nanoparticles were round or similar. The mean particle size,encapsulation efficiency and drug loading of anti-epilepsy peptide nanoparticles were （ 100. 2 ± 2. 45 ） nm, （ 64. 46 ± 1. 34 ）% and （4. 73 ± 0. 32）%respectively. The drug release from nanoparticles appeared consisting of two phases with initial burst release and sustained-release in vitro,and the release rule accorded with Weibull equation. Conclusion The preparation technics is simple and feasible,and the obtained anti-epilepsy peptide nanoparticles has high encapsulation efficiency, high drug loading,small mean diameter and the drug releasing characteristic is sustained in vitro.