谷胱甘肽敏感的巯嘌呤-透明质酸前药的合成及其释药性能
Journal of Wuhan University(Natural Science Edition)（2015）
Abstract
以透明质酸为载体,采用全化学合成法构建谷胱甘肽敏感的巯嘌呤-透明质酸(6-MP-ss-HA)高分子前药,对目标产物的结构进行鉴定,并探讨了物料投料比、温度和反应介质等条件对产率的影响.在30℃下以乙腈为反应介质,且巯嘌呤(6-MP)与I2按摩尔比1∶1投料时,巯嘌呤-ss-巯嘌呤(6-MP-ss-6-MP)的产率可达84.3％.模拟血液和细胞内环境研究该前药对谷胱甘肽的响应性释药性能,结果表明,药物累积释放率与谷胱甘肽浓度正相关,且基本只在细胞内释放药物.
MoreKey words
mercaptopurine (6-MP),hyaluronic acid (HA),mercaptopurine-hyaluronic acid (6-MP-ss-HA),glutathione-sensitive,drug releasing behavior
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