Chen Guo-Jing, Su Ying-Zhen, Hsu Chin, Lo Yu-Lun, Huang Shih-Jer, Ke Jyun-Han, Kuo Yung-Chih, Wang Li-Fang
Department of Medicinal & Applied Chemistry, College of Life Science, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
J Mater Chem B. 2014 Sep 14;2(34):5666-5675. doi: 10.1039/c4tb00543k. Epub 2014 Jul 25.
Pluronic® F127-modified water-dispersible poly(acrylic acid)-bound iron oxide (PF127-PAAIO) nanoparticles have been prepared as diagnostic agents. A blood-brain-barrier penetrating peptide, angiopep-2 (ANG), was further conjugated onto the surface of the PF127-PAAIO (ANG-PF127-PAAIO) for brain targeting. The ANG-PF127-PAAIO shows negligible cell cytotoxicity, better cellular uptake, and higher T-weighted image enhancement than the PF127-PAAIO in U87 cells. Using an ex vivo blood-brain barrier (BBB) model, we showed that the ANG-PF127-PAAIO shows better permeability to bypass the BBB. This is because the ANG-PF127-PAAIO has a dual-targeting ability, recognition of the low-density lipoprotein receptor-related protein and clathrin-mediated receptor on the U87 surface. Thus, the ANG-PF127-PAAIO is a potential nanotheranostic agent for brain dysfunction.
已制备出普朗尼克® F127修饰的水分散性聚（丙烯酸）结合氧化铁（PF127-PAAIO）纳米颗粒作为诊断剂。一种血脑屏障穿透肽血管活性肠肽-2（ANG）进一步偶联到PF127-PAAIO（ANG-PF127-PAAIO）表面用于脑靶向。在U87细胞中，ANG-PF127-PAAIO的细胞毒性可忽略不计，细胞摄取更好，且T加权图像增强效果比PF127-PAAIO更高。使用体外血脑屏障（BBB）模型，我们表明ANG-PF127-PAAIO绕过血脑屏障的通透性更好。这是因为ANG-PF127-PAAIO具有双重靶向能力，可识别U87表面的低密度脂蛋白受体相关蛋白和网格蛋白介导的受体。因此，ANG-PF127-PAAIO是一种用于脑功能障碍的潜在纳米诊疗剂。
