School of Materials Science and Engineering, Key Laboratory of Advanced Technologies of Materials, Ministry of Education, Southwest Jiaotong University, Chengdu 610031, PR China.
Int J Pharm. 2012 Jun 15;429(1-2):113-22. doi: 10.1016/j.ijpharm.2012.03.001. Epub 2012 Mar 8.
The magnetic nanomicelles as a potential platform for dual targeted (folate-mediated and magnetic-guided) drug delivery were developed to enhance the efficiency and veracity of drug delivering to tumor site. The magnetic nanocarriers were synthesized based on superparamagnetic iron oxide nanoparticles (SPIONs), biocompatible Pluronic F127 and poly(dl-lactic acid) (F127-PLA) copolymer chemically conjugated with tumor-targeting ligand-folic acid (FA) via a facile chemical conjugation method. Doxorubicin hydrochloride (DOX·HCl) was selected as a model anticancer drug to investigate the in vitro drug release and antiproliferative effect of tumor cells in vitro and in vivo in the presence or absence of an external magnetic filed (MF) with strength of 0.1T. The Alamar blue assay exhibited that these magnetic nanomicelles possessed remarkable cell-specific targeting in vitro. Additionally this smart system enabling folate receptor-mediated uptake into tumor cells, showed strong responsiveness to MF. The primary in vivo tumor model study, which was carried out in VX2 tumor-bearing male New Zealand white rabbits, demonstrated that the nanomicelles could be guided into tumor site more efficiently by application of MF, and further represented significant therapeutic efficiency to solid tumor.
作为一种潜在的双重靶向（叶酸介导和磁导向）药物输送平台，磁性纳米胶束被开发出来以提高药物输送到肿瘤部位的效率和准确性。磁性纳米载体是基于超顺磁性氧化铁纳米粒子（SPIONs）、生物相容性的 Pluronic F127 和聚（DL-乳酸）（F127-PLA）共聚物合成的，通过简便的化学偶联方法将肿瘤靶向配体叶酸（FA）化学偶联到共聚物上。盐酸多柔比星（DOX·HCl）被选择为模型抗癌药物，以研究在不存在或存在 0.1T 强度的外部磁场（MF）的情况下，纳米胶束在体外和体内的药物释放和体外肿瘤细胞增殖抑制作用。阿马里蓝分析表明，这些磁性纳米胶束在体外具有显著的细胞特异性靶向性。此外，这种智能系统能够使叶酸受体介导的摄取进入肿瘤细胞，并对 MF 表现出很强的响应性。在 VX2 肿瘤荷瘤雄性新西兰白兔中进行的初步体内肿瘤模型研究表明，MF 的应用可以更有效地将纳米胶束引导到肿瘤部位，并进一步表现出对实体瘤的显著治疗效果。
