Key laboratory for Molecular Enzymology and Engineering, the Ministry of Education, College of Life Science, Jilin University, Changchun 130012, China.
Colloids Surf B Biointerfaces. 2013 Oct 1;110:411-8. doi: 10.1016/j.colsurfb.2013.04.038. Epub 2013 May 16.
The aim of this study was to design and synthesize a polymeric nanocarrier system loaded with both superparamagnetic iron oxide nanoparticles (SPIONs) and the anticancer drug evodiamine through a solvent evaporation technique. The hydrodynamic diameter of the prepared SPION-evodiamine-loaded nanocarrier was approximately 261nm, and the drug-loading content and encapsulation efficiency were 8.61±0.73% and 40.36±3.42%, respectively. The nanocarrier exhibited good superparamagnetism and an iron content of approximately 9.34%. In vitro drug release experiments showed a sustained release profile over 70h. Staining with Prussian blue confirmed that the nanocarrier could be effectively internalized into HeLa cells. MTT assays indicated that the SPION-evodiamine-loaded nanocarrier showed cytotoxicity comparable to that of free evodiamine. If an external magnetic field was applied, the SPION-loaded nanocarrier accumulated at the targeted sites and demonstrated a magnetic force-mediated targeting property with the aid of a magnetic field. Furthermore, the SPION-evodiamine-loaded nanocarrier exhibited a much higher in vivo antitumor efficacy than free evodiamine. Together, these results indicate that the SPION-evodiamine-loaded nanocarrier could effectively inhibit tumor growth both in vitro and in vivo with reduced toxicity, and therefore is a promising candidate to achieve enhanced therapeutic efficacy for clinical development.
本研究旨在通过溶剂蒸发技术设计并合成一种载有超顺磁性氧化铁纳米粒子(SPIONs)和抗癌药物吴茱萸碱的聚合物纳米载体系统。所制备的 SPION-吴茱萸碱载药纳米载体的水动力学直径约为 261nm,载药量和包封率分别为 8.61±0.73%和 40.36±3.42%。该纳米载体具有良好的超顺磁性和约 9.34%的铁含量。体外药物释放实验显示出超过 70h 的持续释放曲线。普鲁士蓝染色证实纳米载体可以有效内化进入 HeLa 细胞。MTT 实验表明,SPION-吴茱萸碱载药纳米载体的细胞毒性与游离吴茱萸碱相当。如果施加外部磁场,载有 SPION 的纳米载体将聚集在靶向部位,并在外磁场的帮助下表现出磁力介导的靶向特性。此外,SPION-吴茱萸碱载药纳米载体在体内的抗肿瘤疗效明显高于游离吴茱萸碱。综上所述,这些结果表明,SPION-吴茱萸碱载药纳米载体可以有效抑制体外和体内肿瘤的生长,同时降低毒性,因此是实现临床开发增强治疗效果的有前途的候选物。
Colloids Surf B Biointerfaces. 2013-5-16
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