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首页> 外文期刊>RSC Advances >Preparation of redox-sensitive, core-crosslinked micelles self-assembled from mPEGylated starch conjugates: remarkable extracellular stability and rapid intracellular drug release
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Preparation of redox-sensitive, core-crosslinked micelles self-assembled from mPEGylated starch conjugates: remarkable extracellular stability and rapid intracellular drug release

机译：从Mpegylated淀粉缀合物自组装的氧化还原敏感，核心交联胶束的制备：显着的细胞外稳定性和快速的细胞内药物释放

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An ideal tumor drug delivery platform should offer little release of the drug in a physiological environment and fast release of the drug once endocytosis into the tumor tissues occurs. Therefore, we have developed a new kind of core-crosslinked copolymers (mPEG-St-SeSex) based on mPEGylated starch and diselenide bonds for rapid drug release. The corresponding core-crosslinked analogs mPEG-St-SSx and mPEG-St-CCx copolymers using 3,3'-dithiodipropionic acid and octanedioic acid as crosslinkers, respectively, were synthesized and used as controls. The results displayed that all amphiphilic core-crosslinked copolymers could form micelles with spherical structures in aqueous solution, showing advanced stability compared to non-crosslinked micelles (mPEG-St) in physiologically related and ultra micelle destabilization conditions. The disassembly of micelles triggered by DTT, combined with in vitro drug release assay and intracellular drug release studies using confocal laser scanning microscopy (CLSM), indicated that the DOX-loaded mPEG-St-SeSex micelles showed higher activity and could be more quickly disrupted than the DOX-loaded mPEG-St-SSx and mPEG-St-CCx micelles in reducing environment and subsequently rapidly released drug. These results, in addition to cell cytotoxicity studies, demonstrated that the mPEG-St-SeSex micelles have the potential to develop controlled drug-delivery systems for cancer therapy.
机译：理想的肿瘤药物递送平台应提供药物的释放很少在生理环境中，快速释放药物，一旦内吞作用进入肿瘤组织发生。因此，我们已经开发了一种新的基于mPEGylated淀粉和快速药物释放硒债券核交联共聚物（MPEG-ST-SeSex）的。相应的芯交联的类似物的mPEG-ST-的SSx以及使用3,3'-二硫代二丙酸和辛二酸作为交联剂的mPEG-ST-CCx中共聚物，分别合成并用作对照。结果显示，所有两亲核 - 交联的共聚物可形成具有球形结构的胶束在水溶液中，显示出相对于非交联胶束（MPEG-ST）在生理相关的和超胶束去稳定化条件先进的稳定性。拆卸的由DTT触发胶束，在体外药物释放试验，并使用共聚焦激光扫描显微镜（CLSM）的细胞内药物释放研究，表明结合了装载DOX的mPEG-ST-SeSex胶束显示出较高的活性，并且可以更迅速地破坏比还原环境，并随后迅速释放药物的装载DOX的mPEG-圣-SSX和MPEG-ST-CCx之间胶束。这些结果，除了细胞的细胞毒性研究，证明了对MPEG-ST-SeSex胶束具有开发用于癌症治疗的对照药物输送系统的潜力。

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