卡铂白蛋白微球的制备和体外性质

 目的：制备可生物降解的卡铂白蛋白微球。方法：以白蛋白为载体，用乳化直接加热固化法制备了卡铂白蛋白微球。结果：微球外观呈米黄色，平均粒径58.2μm，药物含量(11.26±0.48)%，包封率(84.5±3.6)%。体外释放具有明显的突释效应，2h后的药物释放符合零级动力学过程。其释放曲线方程为：Q=21.90+8.50t(d),r=0.9958,t₅₀=3d。微球在4℃和37℃贮存3个月，其外观、粒径及含药量均未见明显改变。结论：本法工艺简便，重现性好，所得微球稳定，药物包封率高，体外药物释放符合零级过程，具有较好的临床应用前景。

Preparation of carboplatin-loaded albumin microsphere and its properties in vitro

To prepare bio-degradable albumin microspheres containing carboplatin. METHODS: Bovin serum albumin microspheres containing carboplatin were prepared by using emulsion-direct heat cross linking techniques. RESULTS: The microsphere was yellow, powdery, with a mean diameter of 58.2 μm. The microphere loaded (11.26±0.48)% carboplatin. The trapping efficiency was (84.5±3.6)%. The pattern of drug releasing from the microspheres in vitro fitted to zero order release plot, with an initial burst in the first 2 hours. The releasing rate can be expressed by the follow equation: Q=21.90+8.50 t (d), r=0.995 8. t50=3 d. Stored at 4 ℃ and 37 ℃ respectively for 3 months, the microspheres did not alter much in shape, size and drug content. CONCLUSIONS: This method is simple, reproducible, having high drug trapping efficiency. The microsphere obtained is stable and release drug at a consistant rate in vitro, leading to a prosperity in clinical use.