首页> 外文期刊>Acta biomaterialia >Enhanced antiproliferative activity of carboplatin-loaded chitosan-alginate nanoparticles in a retinoblastoma cell line.
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Enhanced antiproliferative activity of carboplatin-loaded chitosan-alginate nanoparticles in a retinoblastoma cell line.

机译:转基因瘤细胞系中的卡铂加载的壳聚糖藻酸盐纳米粒子的增强抗增殖活性。

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In the present study the potential of carboplatin-loaded chitosan-alginate nanoparticles (CANPs) for the treatment of retinoblastoma was investigated. The carboplatin-loaded CANPs were approximately 300 nm in size, exhibited a high zeta potential of approximately 36 mV and drug encapsulation of approximately 20 wt.%. The CANPs were further characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry and transmission electron microscopy. In vitro release studies revealed fast release of approximately 25% of the drug during the first 24h, followed by sustained release. CANPs demonstrated greater and sustained antiproliferative activity of the drug in a dose- and time-dependent manner (carboplatin IC(50)=0.56 microg ml(-1), carboplatin-loaded CANPs IC(50)=0.004 microg ml(-1)), as well as an enhanced apoptotic effect as compared with the drug in solution in a retinoblastoma cell line (Y79). The higher cytotoxic effect of CANPs may be due to their greater cellular uptake as compared with native carboplatin. It was also demonstrated that clathrin-mediated endocytosis plays a key role in the internalization of CANPs in the Y79 cell line. In conclusion, biodegradable chitosan nanoparticles could be used as an effective ocular drug delivery system for sustained intracellular delivery of carboplatin for the treatment of retinoblastoma.
机译:在本研究中,研究了用于治疗视网膜母细胞瘤的卡铂加载的壳聚糖藻酸盐纳米粒子(CANP)的潜力。装载的卡铂的CANP大约为300nm,表现出大约36mV的高Zeta电位和约20重量%的药物包封。%。通过傅里叶变换红外光谱,差示扫描量热法和透射电子显微镜,进一步表征了CANP。体外释放研究显示在前24小时内快速释放约25%的药物,然后持续释放。 CANP以剂量和时间依赖的方式展示了药物的更大和持续的抗增殖活性(Carboplatin IC(50)= 0.56 microg ML(-1),卡铂加载的CANPS IC(50)= 0.004 microg ml(-1) )以及与视网膜细胞瘤细胞系(Y79)中的药物中的药物相比,以及增强的凋亡效应。与天然卡铂相比,CANPS的细胞毒性效果可能是由于它们具有更大的细胞摄取。还证明了克拉辛介导的内吞作用在Y79细胞系中的CANPS内化中起着关键作用。总之,可生物降解的壳聚糖纳米颗粒可用作有效的眼药递送系统,用于治疗视网膜母细胞瘤的持续细胞内递送卡铂。

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