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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Characterisation, cytotoxicity and apoptosis studies of methotrexate-loaded PLGA and PLGA- PEG nanoparticles
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Characterisation, cytotoxicity and apoptosis studies of methotrexate-loaded PLGA and PLGA- PEG nanoparticles

机译：甲氨蝶呤负载的PLGA和PLGA-PEG纳米颗粒的表征，细胞毒性和凋亡研究

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Methotrexate (MTX) widely used in the treatments of various types of malignancies, but high toxicity and short plasma half-life have limited its use. This study was aimed at developing a polymeric drug delivery system for improving the therapeutic index of this potent drug. To achieve these goals, PLGA and PLGA-PEG nanoparticles were prepared using the emulsification-solvent diffusion technique and were optimized for particle size and entrapment efficiency. The optimum loaded nanoparticles were evaluated by cytotoxicity and their ability to induce apoptosis compared to free drug by examining of caspase-3 activity. The results showed that optimized particles were 182 +/- 14nm and 258 +/- 10nm in size for PLGA-PEG and PLGA nanoparticles, respectively, with an entrapment efficiency of more than 51%. The cytotoxicity experiment showed that the nanoparticles were more effective than pure MTX and increase the activity of caspase-3 in MCF7 and AGS and A549 cell lines.
机译：甲氨蝶呤（MTX）广泛用于治疗各种类型的恶性肿瘤，但是高毒性和短血浆半衰期限制了其用途。这项研究旨在开发一种聚合物药物递送系统，以改善这种有效药物的治疗指数。为了实现这些目标，使用乳化溶剂扩散技术制备了PLGA和PLGA-PEG纳米颗粒，并对其粒度和包封效率进行了优化。通过检测caspase-3活性，通过细胞毒性及其与游离药物相比诱导凋亡的能力评估了最佳负载纳米颗粒。结果表明，PLGA-PEG和PLGA纳米粒子的优化粒径分别为182 +/- 14nm和258 +/- 10nm，包封率超过51％。细胞毒性实验表明，纳米颗粒比纯MTX更有效，并增加了MCF7，AGS和A549细胞系中caspase-3的活性。

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