以大分子右旋糖酐(Dex)栽体,丁二酸酐(SA)为交联剂,二环己基碳化亚胺(DOC)为缩合剂制备右旋糖酐基微凝胶,同步接枝单甲氧基聚乙二醇(mPEG)、偶联羟基喜树碱(HCPT)-丁二酸单酯.结果表明,缩短了反应时间;mPEG-gDex微凝胶偶联HCPT形成了内疏水外亲水的胶束结构,粒径分布在200nm～300nm,可实现对肿瘤组织的被动靶向富集;羟基喜树碱在水中的溶解度由3.9μg/mL提高到400μ.g/mL,水溶性增加了约100倍,有利与生物利用度的提高;在pH=7.4缓冲溶液中的释放符合Rc=100t 1.96/(1166.71+0.08t3,08)动力学方程,20h内偶联物释放HCPT只有20%左右,呈现显著缓释特性.
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