氟尿嘧啶白蛋白磁亚微球的制备及释药特性

Preparation and drug release of fluorouracil albumin magnetic deuto-microspheres

目的:优选以牛血清白蛋白为载体的氟尿嘧啶磁亚微球的制备工艺,并考察其体外释药。方法:以载药量、包封率、平均粒径及形态为考察指标,采用均匀设计法及单因素试验设计法筛选优化磁亚微球的最佳制备工艺,并进一步采用体外动态释药法评价其释药特征。结果:以优化工艺制备的磁亚微球形态良好,平均粒径为(330±21)nm,载药量为(9.5±1.2)%,包封率为(68.3±2.0)%,磁响应性能良好。磁亚微球体外释药规律符合Higuchi方程,具有一定的缓释作用。结论:均匀设计法结合单因素试验设计优化筛选氟尿嘧啶磁亚微球最佳制备工艺科学合理,为制备氟尿嘧啶磁亚微球提供了理论依据。

OBJECTIVE To optimize the preparation of Bovine serum albumin magnetic deuto-microspheres containing flu orouracil （FU-AMDM） and investigate the characteristics of drug release. METHODS Based on the evaluation indicators, such as the drug loading and encapsulation efficiency, the mean diameter and the shape, single factor analysis and uniform de- sign method were used to screen the optimal method of the preparation of FU-AMDM. The constant temperature vibration dial ysis method was carried out to evaluate FU release from FU-AMDM in vitro. RESULTS The shape of optimized products was good. The mean diameter was （330 ± 21）nm. The drug loading and drug trapping efficiency of FU-AMDM were （9. 5 ±1.2） and （68. 27 ± 2. 04）% respectively. The magnetic response was fine. The drug release profile could be described by Higuchi equation, and the sustained release could be observed. CONCLUSION The optimization method was scientific and reasonable and provided theoretical basis for the preparation of FU-AMDM.