汉防己甲素-P LGA纳米粒的制备与体外释放∗

摘要

目的：制备载汉防己甲素的聚乳酸-羟基乙酸共聚物(PLGA)纳米粒,并考察其药物释放行为。方法采用乳化分散溶剂挥发法制备汉防己甲素-PLGA纳米粒,通过改变稳定剂浓度及乳化能量,优化制备工艺。通过包封率和载药量考察其载药特性；研究粒径及不同pH值释放介质对药物释放的影响。结果优化后最佳工艺条件制备的汉防己甲素-PLGA纳米粒平均粒径为(203.4±2.8)nm,表面带负电,呈规则的球形。药物包封率和载药量分别为(67.88±4.27)％及(2.17±0.10)％。体外释放实验显示纳米粒缓慢释药,药物累积释放百分率随粒径减小而增加,且在酸性释放介质中有较高的释放量。结论制备的汉防己甲素-PLGA纳米粒粒径大小均一,包封率高,体外释药表现出较好的缓释效果。%Objective To prepare the PLGA nanoparticles( NPs) loading tetrandrine, investigate in vitro drug release behavior. Methods Tetrandrine loaded PLGA NPs were prepared by the emulsion solvent diffusion method and the preparation process was optimized by changing the stabilizer concentration and emulsion energy. The drug loading and entrapment efficiency were studied to evaluate the drug-loading property.The influence of particles size and pH value of release media on drug release behavior was investigated. Results Nanoparticles in the mean size of(203.4±2.8)nm had spherical shape and showed negative surface charge.Drug loading and entrapment efficiency was(2.17±0.10)% and(67.88±4.27)%, respectively.Tet-PLGA NPs retarded drug release in vitro, the cumulative release percentage was increased with the particle size increasing and it in acidic release medium showed a higher drug release amount. Conclusion Tetrandrine loaded PLGA nanoparticles have good entrapment efficiency, uniform particle size and can retard drug release in vitro.