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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Long circulating PEGylated PLGA nanoparticles of cytarabine for targeting leukemia
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Long circulating PEGylated PLGA nanoparticles of cytarabine for targeting leukemia

机译：阿糖胞苷的长循环聚乙二醇化PLGA纳米颗粒靶向白血病

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摘要

The present investigation was aimed at developing PEGylated PLGA nanoparticles of cytarabine. PLGA Nanoparticles were prepared by modified nanoprecipitation method, optimized for mean particle size (152±6nm) and entrapment efficiency (41.1 ±0.8%) by a 3~2 factorial design. The PEGylated PLGA nanoparticles of cytarabine had a zeta potential of —7.5 ± 1.3 mV and sustained the release of cytarabine for 48 h by Fickian diffusion. The IC_(50) values for L1210 cells were 6.5, 5.3, and 2.2 μM for cytarabine, cytarabine loaded PLGA nanoparticles and cytarabine loaded PLGA-mPEG nanoparticles respectively. Confocal microscopy and flow cytometry showed that the nanoparticles were internalized by the L1210 cells and not simply bound to their surface. Biodistribution studies showed that the PEGylated nanoparticles of cytarabine were present in significantly higher concentrations in blood circulation as well as in brain and bones and avoided RES uptake as compared to the free drug.
机译：本研究旨在开发阿糖胞苷的PEG化PLGA纳米颗粒。 PLGA纳米粒子采用改进的纳米沉淀法制备，通过3〜2因子设计优化了平均粒径（152±6nm）和包封率（41.1±0.8％）。阿糖胞苷的PEG化PLGA纳米颗粒的ζ电位为-7.5±1.3 mV，并通过Fickian扩散持续释放阿糖胞苷48小时。对于阿糖胞苷，阿糖胞苷的PLGA纳米颗粒和阿糖胞苷的PLGA-mPEG纳米颗粒，L1210细胞的IC_（50）值分别为6.5、5.3和2.2μM。共聚焦显微镜和流式细胞术表明，纳米颗粒被L1210细胞内在化，而不是简单地与其表面结合。生物分布研究表明，与游离药物相比，阿糖胞苷的聚乙二醇化纳米颗粒在血液循环以及脑和骨骼中的浓度明显更高，并且避免了RES的吸收。

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