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首页> 外文期刊>Chemistry: A European journal >Enhanced in vitro antitumor efficacy and strong anti-cell-migration activity of a hydroxycamptothecin-encapsulated magnetic nanovehicle
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Enhanced in vitro antitumor efficacy and strong anti-cell-migration activity of a hydroxycamptothecin-encapsulated magnetic nanovehicle

机译：羟基喜树碱包裹的磁性纳米载体的增强的体外抗肿瘤功效和强大的抗细胞迁移活性

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摘要

A 10-hydroxycamptothecin-encapsulated magnetic nanovehicle (HEMN) was fabricated by coencapsulating Fe _3O _4 nanoparticles and 10-hydroxycamptothecin (HCPT) into a micelle core self-assembled from the amphiphilic copolymer methoxy-poly(ethylene glycol)-poly(d,l-lactide-co- glycolide) through a facile dialysis method. A satisfactory drug-loading content of (9.03±0.67) % and a relatively high encapsulation efficiency of (53.52±6.46) % were achieved. In vitro drug release was performed by membrane dialysis and a pH-dependent release behavior was observed. In comparison with free HCPT dissolved in dimethylsulfoxide, HEMNs showed a greatly improved in vitro antitumor efficacy against three different human cancer cell lines-HeLa, A549, and HepG2-and lower IC _(50) values were measured. The mechanism of cell death was investigated, and it was clearly demonstrated that the apoptosis process was triggered. An in vitro wound-healing assay and a transwell assay indicated that HEMNs exerted much stronger activity in inhibiting HeLa cell migration. The cellular uptake of HEMNs in a desired area can be significantly enhanced by an external magnetic field. These results demonstrate HCPT-encapsulated magnetic nanovehicles might have important potential in clinical applications for inhibiting tumor metastasis and for targeted drug delivery.
机译：通过将Fe _3O _4纳米粒子和10-羟基喜树碱（HCPT）共包裹到由两亲共聚物甲氧基-聚（乙二醇）-聚（d，l）自组装的胶束核中，制得了10-羟基喜树碱包裹的磁性纳米载体（HEMN）。 -丙交酯-乙交酯）通过简便的透析方法。获得令人满意的（9.03±0.67）％的载药量和（53.52±6.46）％的相对高的包封效率。通过膜透析进行体外药物释放，观察到pH依赖性释放行为。与溶解在二甲亚砜中的游离HCPT相比，HEMNs对三种不同的人类癌细胞系HeLa，A549和HepG2的体外抗肿瘤功效大大提高，并且IC_（50）值较低。研究了细胞死亡的机制，并且清楚地证明了细胞凋亡过程被触发。体外伤口愈合分析和transwell分析表明HEMNs在抑制HeLa细胞迁移方面发挥了更强的活性。通过外部磁场可以显着增强所需区域中HEMN的细胞吸收。这些结果表明，HCPT封装的磁性纳米载体在临床应用中可能具有重要的潜力，可用于抑制肿瘤转移和靶向药物递送。

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