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N-lauroyl chitosan surface-modified PLGA nanoparticles as carrier for adriamycin to overcome cancer drug resistance

机译:N-月桂酰壳聚糖表面修饰的PLGA纳米粒子作为阿霉素的载体以克服癌症的耐药性

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N-lauroyl chitosan (NLCS) conjugates with different degrees of substitution (DS) of lauroyl group were synthesized and used to prepare surface modified poly(lactic-co-glycolic) acid (NLCS-PLGA) nanoparticles via hydrophobic interaction and ionic bond force. NLCS-PLGA nanoparticles had spherical shape with shell-core structure and exhibited the smallest size and narrowest size distribution when DS of lauroyl group of NLCS was 8.5%. Adriamycin (ADR), as a model antitumor drug, was loaded into NLCS-PLGA nanoaprticles and its initial burst release from PLGA nanoparticles was significantly reduced. MTT assay showed that NLCS-2-PLGA nanoaprticles evidently enhanced cytotoxicity of ADR against drug-resistant breast cancer MCF-7/ADR cells, both compared to free ADR and ADR-loaded PLGA nanoparticles. Moreover, cell-live images showed that the cellular uptake and nuclear location of ADR in MCF-7/ADR cells were significantly enhanced by loading of NLCS-2-PLGA nanoparticles. In conclusion, this novel carrier of anticancer drugs has the potential to overcome drug resistance in cancer cells.
机译:合成了具有不同取代度(DS)的月桂酰基的N-月桂酰壳聚糖(NLCS)共轭物,并通过疏水作用和离子键合力制备了表面改性的聚乳酸-乙醇酸(NLCS-PLGA)纳米粒子。当NLCS的月桂酰基的DS为8.5%时,NLCS-PLGA纳米颗粒为具有壳核结构的球形,并且具有最小的尺寸和最窄的尺寸分布。将阿霉素(ADR)作为模型抗肿瘤药物加载到NLCS-PLGA纳米微囊中,并显着降低了其从PLGA纳米颗粒的初始爆发释放。 MTT分析表明,与游离ADR和载有ADR的PLGA纳米颗粒相比,NLCS-2-PLGA纳米膜明显增强了ADR对耐药性乳腺癌MCF-7 / ADR细胞的细胞毒性。此外,细胞活体图像显示,通过加载NLCS-2-PLGA纳米颗粒,MCF-7 / ADR细胞中ADR的细胞摄取和细胞核位置显着增强。总之,这种新型的抗癌药物载体具有克服癌细胞耐药性的潜力。

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