Hua Xin, Yang Qin, Dong Zhimin, Zhang Jiashuo, Zhang Wanjiang, Wang Qiudong, Tan Shengnan, Smyth Hugh D C
a Division of Bacterial Diseases , State Key Laboratory of Veterinary Biotechnology, Harbin Veterinary Research Institute, Chinese Academy of Agricultural Sciences , Harbin , China.
b Tianjin Animal Science and Veterinary Research Institute , Tianjin , China.
Drug Deliv. 2017 Nov;24(1):511-518. doi: 10.1080/10717544.2016.1256001.
The objective of this study was to describe the magnetic nanoparticle-drug conjugates for improved control of drug delivery and drug release. The widely used anticancer agent Doxorubicin (DOX) was successfully conjugated via amine groups to the carboxylic functional groups coating magnetic nanoparticles (fluidMAG-CMX). Following purification of the nanoparticles, the conjugation of DOX on fluidMAG-CMX was confirmed using FTIR spectroscopy and confocal microscopy. The observed drug loading capacity of DOX was 22.3%. Studies of magnetically triggered release were performed under an oscillating magnetic field (OMF). DOX exhibited a significant release percentage of 70% under an OMF, as compared with the release in enzyme. A magnetic field turn-on and turn-off experiment was also conducted to confirm the control of drug release using this triggered system. In vivo experiments indicated that the tumor-inhibitory rate of CMX-DOX NPs under a magnetic field was higher than the other control groups. According to the toxicity assessments, CMX-DOX NPs were not noticeably toxic to mice at our tested dose.
本研究的目的是描述用于改善药物递送和药物释放控制的磁性纳米颗粒-药物缀合物。广泛使用的抗癌药物阿霉素(DOX)通过胺基成功地与包覆磁性纳米颗粒(fluidMAG-CMX)的羧基官能团偶联。纳米颗粒纯化后,使用傅里叶变换红外光谱(FTIR)和共聚焦显微镜确认了DOX在fluidMAG-CMX上的偶联。观察到DOX的载药量为22.3%。在振荡磁场(OMF)下进行了磁触发释放研究。与在酶中的释放相比,DOX在OMF下的释放率高达70%。还进行了磁场开启和关闭实验,以确认使用该触发系统对药物释放的控制。体内实验表明,磁场作用下CMX-DOX纳米颗粒的抑瘤率高于其他对照组。根据毒性评估,在我们测试的剂量下,CMX-DOX纳米颗粒对小鼠没有明显毒性。