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目的 寻找与DSPE PEG功能相似的表面活性剂 ,以增加脂质体的稳定性 ,改善其体内分布 ,提高靶向性。方法制备了伊文思蓝脂质体 ,考察了胆固醇与磷脂的比例对伊文思蓝脂质体包封率的影响 ;比较了用DSPE PEG、Tween80和Brij35修饰后的伊文思蓝脂质体包封率和在大鼠体内分布状况的变化。结果 伊文思蓝脂质体的包封率最高为 2 5 30 %。用DSPE PEG、Tween80和Brij35修饰后使伊文思蓝脂质体的包封率略有下降 ,但差别不显著 ;体内分布实验结果显示 :修饰后的脂质体在肝、脾和肾中伊文思蓝的浓度均有不同程度的降低 ,脑中伊文思蓝的浓度有所提高 ,而且以Tween80修饰组最显著。结论 DSPE PEG、Tween80和Brij35对伊文思蓝脂质体的包封率影响较小。Brij35对伊文思蓝脂质体的作用与DSPE PEG相似 ,能提高脂质体逃避网状内皮系统吞噬的能力 ;Tween80主要能增加伊文思蓝脂质体在大鼠脑组织中的分布 ,为脑靶向脂质体的研究提供了有益信息
Objective To find a surfactant with similar function to DSPE PEG to increase the stability of liposomes, improve the distribution in vivo and improve the targeting ability. Methods Evans blue liposomes were prepared and the effect of the ratio of cholesterol to phospholipids on the encapsulation efficiency of Evans blue liposomes was investigated. Evans blue liposomes encapsulated with DSPE PEG, Tween80 and Brij35 were compared. Rate and changes in the distribution of the body in rats. Results The highest encapsulation efficiency of Evans blue liposomes was 2530%. The encapsulation efficiency of Evans blue liposome decreased slightly with the modification of DSPE PEG, Tween80 and Brij35, but the difference was not significant. The results of in vivo distribution showed that the modified liposome encapsulated in Evans blue, Blue concentrations were reduced to varying degrees, the brain Evans blue concentration increased, and Tween80 modified group the most significant. Conclusion DSPE PEG, Tween80 and Brij35 have little effect on the encapsulation efficiency of Evans blue liposomes. Brij35 has similar effects on Evans blue liposomes as DSPE PEG, which can enhance the ability of liposomes to evade reticuloendothelial system phagocytosis. Tween80 mainly increases the distribution of Evans blue liposomes in rat brain tissue, Targeted liposome research provides useful information