Wu Bo, Lu Shu-Ting, Deng Kai, Yu Hui, Cui Can, Zhang Yang, Wu Ming, Zhuo Ren-Xi, Xu Hai-Bo, Huang Shi-Wen
Department of Radiology, Zhongnan Hospital of Wuhan University.
Key Laboratory of Biomedical Polymers, Ministry of Education, Department of Chemistry, Wuhan University, Wuhan, People's Republic of China.
Int J Nanomedicine. 2017 Sep 14;12:6871-6882. doi: 10.2147/IJN.S143048. eCollection 2017.
In recent years, there has been increasing interest in developing a multifunctional nanoscale platform for cancer monitoring and chemotherapy. However, there is still a big challenge for current clinic contrast agents to improve their poor tumor selectivity and response. Herein, we report a new kind of Gd complex and folate-coated redox-sensitive lipid-polymer hybrid nanoparticle (Gd-FLPNP) for tumor-targeted magnetic resonance imaging and therapy. Gd-FLPNPs can simultaneously accomplish diagnostic imaging, and specific targeting and controlled release of doxorubicin (DOX). They exhibit good monodispersity, excellent size stability, and a well-defined core-shell structure. Paramagnetic nanoparticles based on gadolinium-diethylenetriaminepentaacetic acid-bis-cetylamine have paramagnetic properties with an approximately two-fold enhancement in the longitudinal relaxivity compared to clinical used Magnevist. For targeted and reduction-sensitive drug delivery, Gd-FLPNPs released DOX faster and enhanced cell uptake in vitro, and exhibited better antitumor effect both in vitro and in vivo.
近年来，人们对开发用于癌症监测和化疗的多功能纳米级平台越来越感兴趣。然而，当前临床造影剂在改善其较差的肿瘤选择性和反应性方面仍然面临巨大挑战。在此，我们报道了一种新型的钆配合物和叶酸包被的氧化还原敏感脂质-聚合物杂化纳米颗粒（Gd-FLPNP），用于肿瘤靶向磁共振成像和治疗。Gd-FLPNPs能够同时完成诊断成像以及阿霉素（DOX）的特异性靶向和控释。它们表现出良好的单分散性、出色的尺寸稳定性以及明确的核壳结构。基于钆-二乙烯三胺五乙酸-双十六胺的顺磁性纳米颗粒具有顺磁性，其纵向弛豫率比临床使用的马根维显提高了约两倍。对于靶向和还原敏感的药物递送，Gd-FLPNPs在体外更快地释放DOX并增强细胞摄取，并且在体外和体内均表现出更好的抗肿瘤效果。
