A new type of reduction- and pH-mediated glyco-polymeric micelles was synthesized for the antitumor drug doxorubicin (DOX) delivery in this study. The micelles were constructed by a diblock copolymer (MH-S-S-AcMH) with a disulfide linkage between hydrophilic block maltoheptaose (MH) and hydrophobic block acetalated maltoheptaose (AcMH). The experimental results showed that the amphiphilic MH-S-S-AcMH with 20 nm average size could self-assemble into micelles under physiological conditions and rapidly release the conjugated drug DOX when exposed to weakly acidic (pH = 5) and reductive (10 mM DTT) environment. Fluorescence microscopy detection indicated that drug carriers can be endocytosed effectively, making the anticancer agents flow into cells and suppress the growth of HeLa tumor cells. Compared with DOX at higher dosage and MH-S-S-AcMH micelles which are non-toxic to tumor cells, cytotoxicity assays manifested that the DOX-loaded MH-S-S-AcMH micelles exhibited better toxicity to HeLa tumor cells. According to these results, the copolymer mentioned above as practically non-toxic, highly stable, novel reduction- and pH-mediated glyco-polymeric micelles could be employed in improving drug delivery efficiency and enhancing anticancer efficacy.

中文翻译：

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由基于麦芽七糖的两亲物构建的二嵌段共聚物糖基萘酚，用于还原和pH介导的细胞内药物传递†

在本研究中，合成了一种新型的还原和pH介导的糖聚合物胶束，用于递送抗肿瘤药阿霉素（DOX）。通过在亲水性嵌段麦芽七糖（MH）和疏水性嵌段缩醛化麦芽七糖（AcMH）之间具有二硫键的二嵌段共聚物（MH-SS-AcMH）构造胶束。实验结果表明，在生理条件下，平均粒径为20 nm的两亲性MH-SS-AcMH可以自组装成胶束，并在弱酸性（pH = 5）和还原性（10 mM DTT）下迅速释放结合药物DOX。环境。荧光显微镜检测表明，药物载体可以被有效地内吞，使抗癌药流入细胞并抑制HeLa肿瘤细胞的生长。与较高剂量的DOX和对肿瘤细胞无毒的MH-SS-AcMH胶束相比，细胞毒性试验表明，装载DOX的MH-SS-AcMH胶束对HeLa肿瘤细胞表现出更好的毒性。根据这些结果，可以将上述作为实际上无毒，高度稳定，新颖的还原和pH介导的糖聚合物胶束的共聚物用于改善药物递送效率和增强抗癌功​​效。