Drug-loaded magnetic nanoparticles have been developed because of the advantages of specific drug targeting in cancer treatment. Pemetrexed (PEM) is a multi-targeting antifolate agent that is effective for the treatment of many cancers, for example, non-small cell lung cancer. Here, PEM loaded magnetic O-carboxymethyl chitosan (O-CMC) nanoparticles were prepared to deliver PEM on tumor tissue with an external magnetic field. The modification of chitosan to O-CMC was confirmed by FTIR analysis. Nanoparticle synthesis was performed via ionic gelation method. The diameter of magnetic O-CMC nanoparticles (MCMC) was found to be 130.1 ± 22.96 nm. After PEM loading, diameter was found to be 123.9 ± 11.42 nm. The drug release of PEM loaded MCMC (PMCMC) was slower in physiological medium than in acidic medium. A549-luc-C8 and CRL5807 cell lines were used for MTT test which showed that IC50 values of nanoparticles were lower than PEM. The antitumor efficiency of PMCMC in xenograft tumor model was examined with in vivo imaging system (IVIS) and caliper and with hematological analyses. In vivo studies revealed that PMCMC had targeted antitumor activity in A549-luc-C8-tumor-bearing mice compared to PEM. As a result, it was suggested that PMCMC have great potential for the treatment of non-small cell lung cancer.

中文翻译：

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磁性纳米颗粒对培美曲塞的递送：设计，表征，体外和体内评估。

由于在癌症治疗中靶向特定药物的优势，已经开发了载有药物的磁性纳米粒子。培美曲塞（PEM）是一种多靶点抗叶酸药物，可有效治疗多种癌症，例如非小细胞肺癌。在此，制备了PEM负载的磁性O-羧甲基壳聚糖（O-CMC）纳米颗粒，以在具有外部磁场的肿瘤组织上递送PEM。通过FTIR分析证实了壳聚糖向O-CMC的修饰。纳米粒子的合成通过离子凝胶法进行。发现磁性O-CMC纳米颗粒（MCMC）的直径为130.1±22.96 nm。加载PEM后，发现直径为123.9±11.42 nm。载有PEM的MCMC（PMCMC）在生理介质中的释放比在酸性介质中的释放慢。A549-luc-C8和CRL5807细胞系用于MTT测试，结果表明纳米粒子的IC50值低于PEM。通过体内成像系统（IVIS）和测径仪以及血液学分析检查了PMCMC在异种移植肿瘤模型中的抗肿瘤效率。体内研究显示，与PEM相比，PMCMC在具有A549-luc-C8肿瘤的小鼠中具有靶向的抗肿瘤活性。结果表明，PMCMC在治疗非小细胞肺癌方面具有巨大潜力。