新型汉防己甲素纳米微球的制备及性质研究

Novel nanoparticles of tetradrine:preparation and properties

目的:以自行合成的mPEG-PCL(单甲氧基聚乙二醇-聚己内酯)为原料,制备负载汉防己甲素的高分子纳米微球,并全面考察其性质。方法:通过开环聚合法,制备mPEG-PCL两嵌段聚合物,采用优化的o/w乳化扩散/挥发法,制备负载汉防己甲素的纳米粒子。优化制备工艺并考察载体的结构、分子量,纳米粒子的形态、粒径分布、体外释药特性等性质。结果:通过开环聚合法合成mPEG-PCL两嵌段聚合物,测定分子量和设计分子量相近。通过乳剂-挥发法制备的空白粒子呈规整的球形,在冻干前后的平均粒径为(272.6±3.2)nm及(285.8±4.2)nm,载药粒子在冻干前后的粒径分别为(281.5±3.8)nm及(287.6±6.0)nm。汉防己甲素的最高载药量为14.38%。体外释放实验显示,载药粒子具有缓释特征,在6h、12h、48h分别释放48%、58%、71%。结论:本文报道的汉防己甲素载药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 tetradrine （Tet） - loaded nanoparticles with di - block copolymer mPEG - PCL, and evaluate their properties. Methods ： mPEG - PCL was synthesized by ring - opening polymerization method and the nanoperticles were prepared by the optimized o/w emulsion - evaporation method. Chemical structure and molecular weight of the copolymer and physical properties of the nanoparticles such as morphology, particle size, drug loadings etc. Were studied comprehensively. Results： mPEG - PCL was synthesized with the desired molecular weight. The nanoparticles are global with good storage stability. The diameter of blank nanoparticles was （272.6 ±3.2 ） nm and （285.8 ± 4.2） nm before and after freeze - dry respectively. The diameter of Tet - loaded nanoparticles was （ 281.5 ± 3.8） nm and （287.6 ~± 6.0 ） nm before and after freeze - dry respectively. The maxium drug loading content was 14.38%. In vitro release study demonstrated the sustained release of Tet from Tet - loaded nanoparticles with the release of 48 % , 58 % and 71% percentage of total drug at 6h, 12h, and 48h, respectively. Conclusion： Tet - loaded nanoparticles reported in the current report showed a good sustained release pattern,which featured it a potential application in cancer treatment.