新型左旋棉酚纳米微球的制备及性质研究

Studies of the preparation and properties of new nanoparticles of(-)-gossypol

目的:以mPEG-mal(单甲氧基聚乙二醇-马来酰亚胺)为原料,制备负载左旋棉酚的高分子纳米微球,并全面考察其性质。方法:通过O/W乳化扩散/挥发法,制备负载左旋棉酚的纳米粒子,优化制备工艺并考察纳米粒子的形态、粒径分布、体外释药特性及稳定性等性质。结果:通过乳剂-挥发法制备的空白粒子呈规整的球形,载药粒子的粒径为(65.1±15.2)nm,左旋棉酚的平均载药量为(37.5±0.3)%。体外释放实验显示,载药粒子具有缓释特征,在12h、24h、10d分别释放7.2%、14.6%、87.7%,并且稳定性良好。结论:本研究制备的左旋纳米微球具有一定的缓释特征,具有良好的应用前景和价值。

Objective：To prepare（-）-gossypol-loaded nanoparticles with mPEG-maleimide,and evaluate their properties.Methods： The nanoparticles were prepared by O/W emulsion-evaporation method.Optimize the preparation technology.The physical properties of nanoparticles such as morphology,particle size,drug release,storage stability were studied comprehensively.Results： The blank nanoparticles were regular global shape.The diameter of（-）-gossypol loaded nanoparticles was（65.1±15.2） nm.The average drug loading content was（37.5 ±0.3）%.In vitro release study demonstrated the sustained release of（-）gossypol from（-）gossypol-loaded nanoparticles with the release of 7.2%,14.6% and 87.7% percentage of total drug at 12h,24h,and 10d,respectively.（-）-Gossypol loaded nanoparticles have good storage stability.Conclusion：（-）-Gossypol-loaded nanoparticles reported in the current report showed a good sustained release property,which featured it a potential application in cancer treatment.