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首页> 外文期刊>RSC Advances >Reduction-responsive core-crosslinked micelles based on a glycol chitosan–lipoic acid conjugate for triggered release of doxorubicin
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Reduction-responsive core-crosslinked micelles based on a glycol chitosan–lipoic acid conjugate for triggered release of doxorubicin

机译：基于二甲酸释放的二甲酸脱甲酸辣椒酸缀合物的减少响应核交联胶束

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Reduction-responsive core-crosslinked micelles were developed based on a glycol chitosan–lipoic acid (GC–LA) conjugate and used for triggered release of doxorubicin (DOX). The substitution degree of GC–LA was 8.3 lipoic acid groups per 100 sugar units of glycol chitosan. GC–LA could form nanoscaled micelles in aqueous solution, wherein the critical micelle concentration (CMC) of 0.081 mg mL ~(?1) was determined. Furthermore GC–LA micelles can be crosslinked by a catalytic amount of dithiothreitol. The mean diameter of DOX-loaded core-crosslinked GC–LA (DOX-GC–LA/cc) micelles increased from 305 to 408 nm as the DOX-loading content increased from 6.03% to 10.74%. DOX-loaded crosslinked micelles demonstrated obvious reduction-triggered destabilization. DOX release from non-crosslinked GC–LA micelles was 87.6% for up to 96 h, whereas 25.3% of DOX release from DOX-GC–LA/cc micelles was observed in phosphate buffered saline (PBS, pH 7.4). Notably, in the presence of a 20 mM GSH-containing environment, accelerated DOX release from DOX-GC–LA/cc micelles was found. The blank micelles had low cytotoxicity in vitro , and DOX-GC–LA/cc micelles demonstrated intracellular redox-responsive characteristics in A549 cancer cells. These results suggested that GC–LA core-crosslinked micelles could be promising carriers for anticancer drug delivery.
机译：基于二醇壳聚糖 - 硫辛酸（GC-LA）缀合物开发还原响应核交联胶束，并用于触发多柔比星（DOX）的释放。 GC-LA的取代度为每100个糖壳聚糖的糖单位为8.3个硫辛酸基团。 GC-LA可以在水溶液中形成纳米级胶束，其中测定临界胶束浓度（CMC）的0.081mg mL〜（α1）。此外，GC-La胶束可以通过催化量的二硫醇交联。随着DOx-Lapuction含量从6.03％增加到10.74％，DOx载核交联的GC-LA（DOX-GC-LA / CC）胶束的平均直径从305升至408nm。 Dox加载的交联胶束表现出明显的减少触发的稳定性。从非交联的GC-La胶束中的DOX释放可为高达96小时，而在磷酸盐缓冲盐水（PBS，pH7.4）中观察到从DOX-GC-LA / CC胶束的DOX释放的25.3％。值得注意的是，在含20mm的GSH的环境存在下，发现来自DOX-GC-LA / CC胶束的加速DOX释放。空白胶束在体外具有低细胞毒性，并且DOX-GC-LA / CC胶束在A549癌细胞中表现出细胞内氧化还原响应特性。这些结果表明GC-LA核交联胶束可能是抗癌药物递送的有前途的载体。

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