pH敏感型K5多糖-阿霉素前体药物的制备及其性能

Preparation and Property Study of the pH-Sensitive K5 Polysaccharide-Doxorubicin Prodrug

DOI：10.3969/j.issn.1673-1689.2015.06.011

中文关键词: K5多糖 前体药物 pH敏感 药物传递

英文关键词: K5 polysaccharide, prodrug, pH-sensitive, drug delivery

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中文摘要:

利用肝素前体K5多糖，通过腙键（Hydrazone bond）连接抗肿瘤药物阿霉素（DOX），制备具有pH敏感性的K5-hydrazone-DOX（KHD）前体药物。对其载药量、形貌和体外药物释放等性质进行了研究，并通过HeLa细胞对其体外细胞毒性和细胞摄取进行了评价。结果表明，所制备的KHD前体药物中，DOX质量分数为18.0%。药物释放结果显示，KHD前体药物在pH 5.0条件下对DOX的释放率远高于pH 7.4条件下的释放率，具有明显的pH响应性。细胞实验表明，KHD前体药物可迅速被细胞摄取，并且具有肿瘤细胞抑制作用。本研究结果表明，KHD是一种有潜在应用价值的抗肿瘤前体药物。

英文摘要:

In this study, K5 polysaccharide (heparosan) was conjugated with anticancer drug DOX via hydrazone bond to obtain pH-sensitive K5-hydrazone-DOX (KHD) prodrug. The drug loaded capacity, morphology, and in vitro drug release were investigated. Its in vitro cytotoxicity and cellular uptake against HeLa cells were also evaluated. The results showed that the DOX content of KHD is 18.0%. The release rate of DOX at pH 5.0 was much faster than that at pH 7.4, revealing a pH-triggered release manner. The KHD prodrug could achieve intracellular delivery and showed effective cytotoxicity in vitro. This study indicates that the KHD prodrug may be a potential candidate for cancer therapy.

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