肺靶向顺铂白蛋白微球的研究

STUDIES ON CISPLATINUM ALBUMIN MICROSPHERES FOR LUNG TARGETING

按正交设计筛选了用乳化一化学交联法制备肺靶向顺铂白蛋白微球的最佳制备工艺，并对微球的质量、稳定性、体内分布、动力学特性和安全性进行了系统研究。结果：微球表面圆整，平均粒径为１３．１３±３．５５μｍ，药物包裹率为２１．６２％，释药特性符合双相动力学方程；微球在三种条件下贮放了３个月质量稳定；静脉注入小鼠体内，１５ｍｉｎ分布达高峰，９７．５２％浓集于肺部，２～３ｄ内基本清除，在肺器官中的动力学特性可用二室开放性模型描述；肺器官病理切片观察，微球对肺组织无病理性损伤。

An optimum procedure was established by orthogonal test preparing cisplatinum albumin microspheres(CDDP-BSA-MS)with emulsion-chemical cross-linking.The quality,stability ,distribution in vivo,kinetic characteristics and safety of the albumin microspheres were studied.The results showed that the surface was regular,the mean size was l3.13士3.55 μm,embedding ratio was 21.62%and the release characteristics in vitro were in accord with“biphase kinetics equatio The stability of the albumin microspheres was good after three months storage,The microspheres accumulated almost entirely in the lung l5 minutes after intravenous injection to mice。The total amount in the lung was about 97%of the injected dose at the peak concentration,Two-compartmental model can be used to describe the regulation of the pharmacokinetics of albumin microspheres in lung.Observation of the lung slice of mice;showed no pathological damage。