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首页> 外文期刊>RSC Advances >Functional block copolymer nanocarriers for anticancer drug delivery
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Functional block copolymer nanocarriers for anticancer drug delivery

机译：用于抗癌药物递送的功能嵌段共聚物纳米载体

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摘要

Polymer-based nanocarriers for anticancer drug delivery bearing "clickable", biodegradable, pH-sensitive and subcellular targeting functions were designed and successfully obtained. Firstly, well-defined functional amphiphilic diblock copolymers were synthesized applying a multistep controlled polymerization and modification procedure. As a result, copolymers comprising alkyne-end functionalized biodegradable poly(D,L-lactide) and polycationic poly(N,N-dimethylaminoethyl methacrylate) blocks were obtained. The latter blocks were additionally functionalized with subcellular targeting triphenylphosphonium cations. The amphiphilic block copolymers self-associated in aqueous media into nanosized functional micelles that were able to incorporate the natural anticancer drug curcumin into their biodegradable cores. The in vitro cytotoxicity evaluation of block copolymer micelles indicated a low intrinsic inhibitory potential on the proliferation of different human cell lines. More importantly, the drug-loaded nanocarriers demonstrated an obvious ability to induce apoptosis and exhibited more prominent inhibition of the NF-kB transcription factor in cancer cell lines and their drug-resistant analogues, as compared to the free drug. The obtained results are optimistic for potential application of the functional block copolymers in nanomedicine.
机译：基于聚合物的抗癌药物递送的纳米载体，设计并成功地设计了“可点击”，可生物降解，pH敏感和亚细胞靶向功能。首先，合成施加多态控制聚合和改性程序的合成明确的官能两亲二嵌段共聚物。结果，得到了包含烷烃末端官能化可生物降解的聚（D，L-丙交酯）和聚阳离子聚（N，N-二甲基氨基甲基甲基丙烯酸酯）嵌段的共聚物。用亚细胞靶向三苯基鏻阳离子另外官能化后一块。在含水介质中自相关的两亲嵌段共聚物成能够将天然抗癌药物姜黄素掺入其可生物降解的核心中的纳米型官能胶束中。嵌段共聚物胶束的体外细胞毒性评价表明了不同人细胞系的增殖的低固有抑制潜力。更重要的是，载有药物的纳米载体表现出诱导凋亡的能力明显并表现出在癌细胞系和它们的药物抗性类似物的NF-kB的转录因子的更突出的抑制，与游离药物。得到的结果对于纳米杂种中的官能嵌段共聚物的潜在施加持乐观态度。

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