树枝状大分子改性聚乙二醇-7-乙基-10-羟基喜树碱聚合物的制备

Preparation of dendrimer modified polyethylene glycol-SN-38

目的:制备树枝状大分子改性聚乙二醇(PEG)-7-乙基-10-羟基喜树碱(SN-38)聚合物,并对聚合物的制备条件、包封率、载药量、粒径表征进行了考察。方法:采用新的"酸酐法"合成了树枝状改性大分子PEG,以树枝状改性大分子PEG为载体材料,SN-38为药物制备树枝状大分子改性聚乙二醇-SN-38聚合物。结果:采用超声波时间为4 h,载体与SN-38质量比为1∶4时,所制备的聚合物有较高包封率、载药量。从粒径分布图可知,聚合物颗粒分布在30 nm和150 nm左右相对集中。结论:所选的处方工艺稳定可靠,具有很大的应用前景。

Objective： Using dendrimer modified polyethylene glycol as a matrix and SN-38 as an antitumor agent,the conjuate were prepared. The ultrasonic time,size distribution,drug loading,entrapment efficiency of dendrimer modified polyethylene glycol-SN-38 were studied. Methods： A novel divergent approach was developed with a new＂anhydride method＂for the synthesis of dendrimer modified polyethylene glycol. Results： The results showed that the conjuate had high drug loading and entrapment efficiency when the ultrasonic time was 4 hours and the ratio of dendrimer modified polyethylene glycol： SN-38 was 1∶ 4. The size distribution of the conjuate were 30 nm to 150 nm. Conclusion： The formulation technology was feasible and stable with good application prospects.