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目的 研究两种方法制备的葡聚糖 表柔比星偶合物的稳定性及体外细胞毒活性。方法 采用高碘酸钠氧化法制备聚醛基葡聚糖 表柔比星偶合物 (PAD EPR) ,将葡聚糖羧甲基化后制备腙健连接的羧甲基葡聚糖 表柔比星偶合物 (CMD EPR)。结果 PAD EPR的载药量为 1∶4,CMD EPR的载药量为 1∶10 ;二者在中性条件下均比较稳定 ,4℃贮存 70d ,药物偶合率都在90 %以上。偶合物的体外细胞毒性比游离药物有所下降 ,游离药物对正常细胞的毒性高于对肿瘤细胞的毒性 ,CMD EPR对肿瘤细胞的毒性高于对正常细胞的毒性 ,PAD EPR对两种细胞的毒性没有差异。结论 CMD EPR优于PAD EPR
Objective To study the stability and in vitro cytotoxicity of dextran epirubicin conjugates prepared by the two methods. Methods PAD EPR was prepared by oxidation of sodium periodate and carboxymethyl dextran was carboxymethylated to prepare hydrazone-linked carboxymethyl dextran epirubicin Conjugate (CMD EPR). Results The drug loading of PAD EPR was 1: 4 and the drug load of CMD EPR was 1:10. Both of them were stable in neutral condition and stored at 4 ℃ for 70 days. The coupling rate of drug was above 90%. The cytotoxicity of the conjugate in vitro was lower than that of the free drug, the toxicity of the free drug to normal cells was higher than that to the tumor cells, the toxicity of CMD EPR to tumor cells was higher than that to normal cells, No difference in toxicity. Conclusion CMD EPR is better than PAD EPR