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首页> 外文期刊>Biomaterials Science >Enhanced endocytosis of acid-sensitive doxorubicin derivatives with intelligent nanogel for improved security and efficacyt
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Enhanced endocytosis of acid-sensitive doxorubicin derivatives with intelligent nanogel for improved security and efficacyt

机译：智能纳米凝胶增强了酸敏感性阿霉素衍生物的内吞作用，提高了安全性和功效

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Three derivatives of doxorubicin (DOX) were prepared by modifying DOX with succinic anhydride, cisaconitic anhydride and 2,3-dimethylmaleic anhydride, generating acid-insensitive succinyl-DOX (SAD), acid-sensitive cis-aconityl-DOX (CAD) and 2,3-dimethylmaleyl-DOX (DAD) respectively. The pH and reduction dual-responsive methoxy poly(ethylene glycol)-poly(L-lysine-co-L-cystine) nanogel was employed to encapsulate the DOX derivatives. In vitro release studies showed that drug release could be accelerated in the intracellular acidic and reductive conditions. Confocal laser scanning microscopy and flow cytometry results demonstrated that an enhanced intracellular drug release was observed in glutathione monoester pretreated HeLa cells (a human cervical cell line). The DOX derivatives exhibited a lower accumulation in the nuclei than DOX. Moreover, the CAD and DAD-loaded nanogels showed a comparable anti-proliferative activity to the DOX-loaded nanogel against HeLa and HepG2 cells (a human hepatoma cell line). As a comparison, the SAD-loaded nanogel almost never inhibited cellular proliferation. The above results suggested that the pH and reduction dual-responsive nanogel can efficiently deliver acid-sensitive DOX derivatives into the nuclei of cancer cells for minimizing the side effects and enhancing the inhibition of cellular proliferation.
机译：通过用琥珀酸酐，顺式乌头酸酐和2,3-二甲基马来酸酐对DOX进行修饰，生成对酸不敏感的琥珀酰-DOX（SAD），对酸敏感的顺式-丙烯酰基-DOX（CAD）和2制备了阿霉素的三种衍生物。 ，3-二甲基马来基-DOX（DAD）。 pH和还原双响应甲氧基聚（乙二醇）-聚（L-赖氨酸-co-L-胱氨酸）纳米凝胶被用来封装DOX衍生物。体外释放研究表明，在细胞内酸性和还原性条件下，药物释放可以加速。共聚焦激光扫描显微镜和流式细胞仪结果表明，在谷胱甘肽单酯预处理的HeLa细胞（人宫颈细胞系）中观察到细胞内药物释放增强。 DOX衍生物在核中的积累低于DOX。此外，载有CAD和DAD的纳米凝胶对载有DOX的纳米凝胶具有抗HeLa和HepG2细胞（人肝癌细胞系）的抗增殖活性。相比之下，加载SAD的纳米凝胶几乎从未抑制细胞增殖。上述结果表明，pH和还原双反应纳米凝胶可以有效地将酸敏感性DOX衍生物递送至癌细胞的细胞核中，以最小化副作用并增强对细胞增殖的抑制。

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