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一种用于制备具有增强的体内治疗效果的诊疗载体的新型胶束形成材料。

A novel micelle-forming material used for preparing a theranostic vehicle exhibiting enhanced in vivo therapeutic efficacy.

作者信息

Chen Hsiao-Ping, Chen Ming-Hong, Tung Fu-I, Liu Tse-Ying

机构信息

†Institute of Biomedical Engineering, National Yang-Ming University, Taipei, Taiwan, R.O.C.

‡Division of Neurosurgery, Department of Surgery, Taipei Tzu Chi Hospital, Taipei, Taiwan, R.O.C.

出版信息

J Med Chem. 2015 May 14;58(9):3704-19. doi: 10.1021/jm501996y. Epub 2015 May 1.

Abstract

A new micelle-forming material, folic acid-conjugated carboxymethyl lauryl chitosan (FA-CLC), and superparamagnetic iron oxide (SPIO) nanoparticles were used for preparing an imaging-guided drug vehicle (the FA-CLC/SPIO hybrid micelle) that demonstrates targeted delivery, imaging, and controlled release of hydrophobic agents. We found that the ratio of viable normal cells to tumor cells was increased prominently after delivery of camptothecin (CPT)-loaded FA-CLC/SPIO micelles and therapeutic sonication. In addition, a magnetic field could enhance the tumor-targeting effect of FA-CLC/SPIO micelles. Therefore, after sequential administration of magnetic attraction to CPT-loaded FA-CLC/SPIO micelles, and therapeutic sonication, the in vivo therapeutic efficacy of CPT was markedly enhanced. However, a nonfocused magnetic field could enhance the undesirable accumulation of iron-containing vehicles in the liver if the tumor (i.e., magnetic attraction site) is near the liver. We propose that magnetic attraction must be carefully applied, far from the liver.

摘要

一种新型的胶束形成材料,叶酸共轭羧甲基月桂基壳聚糖(FA-CLC)和超顺磁性氧化铁(SPIO)纳米颗粒被用于制备一种成像引导药物载体(FA-CLC/SPIO混合胶束),该载体可实现疏水性药物的靶向递送、成像及控释。我们发现,负载喜树碱(CPT)的FA-CLC/SPIO胶束给药并进行治疗性超声处理后,存活的正常细胞与肿瘤细胞的比例显著增加。此外,磁场可增强FA-CLC/SPIO胶束的肿瘤靶向作用。因此,对负载CPT的FA-CLC/SPIO胶束依次施加磁吸引和治疗性超声处理后,CPT的体内治疗效果明显增强。然而,如果肿瘤(即磁吸引部位)靠近肝脏,非聚焦磁场会增强含铁载体在肝脏中的不良蓄积。我们建议,必须谨慎应用磁吸引,使其远离肝脏。

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