School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, PR China.
Biomaterials. 2013 Dec;34(37):9666-77. doi: 10.1016/j.biomaterials.2013.08.049. Epub 2013 Sep 10.
Recently, fullerene and fullerene derivatives owning to their highly enriched physical and chemical properties have been widely explored for applications in many different fields including biomedicine. In this study, iron oxide nanoparticles (IONPs) were decorated onto the surface of fullerene (C60), and then PEGylation was performed to improve the solubility and biocompatibility of C60-IONP, obtaining a multi-functional C60-IONP-PEG nanocomposite with strong superparamagnetism and powerful photodynamic therapy capacity. Hematoporphyrin monomethyl ether (HMME), a new photodynamic anti-cancer drug, was conjugated to C60-IONP-PEG, forming a C60-IONP-PEG/HMME drug delivery system, which demonstrated an excellent magnetic targeting ability in cancer therapy. Compared with free HMME, remarkably enhanced photodynamic cancer cell killing effect using C60-IONP-PEG/HMME was realized not only in a cultured B16-F10 cells in vitro but also in an in vivo murine tumor model due to 23-fold higher HMME uptake of tumor and strong photodynamic activity of C60-IONP-PEG. Moreover, C60-IONP-PEG could be further used as a T2-contrast agent for in vivo magnetic resonance imaging. Our work showed C60-IONP-PEG/HMME had a great potential for cancer theranostic applications.
最近，富勒烯及其衍生物由于其丰富的物理和化学性质而被广泛探索应用于许多不同的领域，包括生物医药。在这项研究中，氧化铁纳米粒子（IONPs）被修饰到富勒烯（C60）的表面，然后进行聚乙二醇化（PEGylation）以提高 C60-IONP 的溶解度和生物相容性，得到具有强超顺磁性和强大光动力治疗能力的多功能 C60-IONP-PEG 纳米复合材料。血卟啉单甲醚（HMME），一种新的光动力抗癌药物，被共轭到 C60-IONP-PEG 上，形成 C60-IONP-PEG/HMME 药物递送系统，该系统在癌症治疗中表现出优异的磁靶向能力。与游离 HMME 相比，使用 C60-IONP-PEG/HMME 不仅在体外培养的 B16-F10 细胞中，而且在体内小鼠肿瘤模型中都实现了显著增强的光动力抗癌细胞杀伤效果，这是由于肿瘤中 HMME 的摄取增加了 23 倍，并且 C60-IONP-PEG 具有很强的光动力活性。此外，C60-IONP-PEG 可以进一步用作体内磁共振成像的 T2 造影剂。我们的工作表明，C60-IONP-PEG/HMME 在癌症治疗应用方面具有很大的潜力。
