Acid-degradable gadolinium-based nanoscale coordination polymer： A potential platform for targeted drug delivery and potential magnetic resonance imaging  

作　　者：Zhimei He  Penghui Zhang  Yan Xiao  Jingjing Li  Fang Yang  Yang Liu  Jian-Rong Zhang  Jun-Jie Zhu 

机构地区：[1]State Key Laboratory of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering Nanjing University Nanjing China [2]The Key Laboratory of Biomedical Information Engineering of the Ministry of Education, School of Life Science and Technology, Bioinspired Engineering and Biomechanics Center (BEBC) Xi’an Jiaotong University Xi’an China [3]School of Medical Imaging Xuzhou Medical University Xuzhou China [4]State Key Laboratory of Bioelectronics, Jiangsu Key Laboratory for Biomaterials and Devices, School of Biological Sciences and Medical Engineering Southeast University Nanjing China

出　　处：《Nano Research》2018年第2期929-939,共11页纳米研究（英文版）

摘　　要：During conventional chemotherapy for cancer, nonspecific drug distribution, which causes serious side effects in normal tissues, is a serious limitation. Thus, it is desirable to develop a tumor or intracellular microenvironment-responsive nanosystem for targeted and on-demand drug release. In the present study, we engineered an intelligent pH-activatable nanosystem, in which a gadolinium- doxorubicin-loaded nanoscale coordination polymer （Gd-Dox NCPs） was the core and hyaluronic acid was the targeting shell. Taking advantage of CD44 receptor-mediated recognition, the nanoparticles were internalized selectively into human cervical carcinoma （HeLa） cells, and trapped within acidic compartments where the fluorescence of Dox recovered, along with the acid dismantling of the Gd NCPs, allowing real-time monitoring of drug release. In vitro experiments also showed that the Gd NCPs present enhanced T1 signals after acid-triggered degradation, suggesting their potential use as contrast agents for magnetic resonance imaging. Such nanocarriers, which feature high biodegradation, selective targeting ability, and rapid response to stimulus, demonstrated enhanced therapeutic efficacy in targeted cancer cells and ＂turned on＂T1 signals in vitro, showing great promise for diagnosis and treatment.During conventional chemotherapy for cancer, nonspecific drug distribution, which causes serious side effects in normal tissues, is a serious limitation. Thus, it is desirable to develop a tumor or intracellular microenvironment-responsive nanosystem for targeted and on-demand drug release. In the present study, we engineered an intelligent pH-activatable nanosystem, in which a gadolinium- doxorubicin-loaded nanoscale coordination polymer （Gd-Dox NCPs） was the core and hyaluronic acid was the targeting shell. Taking advantage of CD44 receptor-mediated recognition, the nanoparticles were internalized selectively into human cervical carcinoma （HeLa） cells, and trapped within acidic compartments where the fluorescence of Dox recovered, along with the acid dismantling of the Gd NCPs, allowing real-time monitoring of drug release. In vitro experiments also showed that the Gd NCPs present enhanced T1 signals after acid-triggered degradation, suggesting their potential use as contrast agents for magnetic resonance imaging. Such nanocarriers, which feature high biodegradation, selective targeting ability, and rapid response to stimulus, demonstrated enhanced therapeutic efficacy in targeted cancer cells and ＂turned on＂T1 signals in vitro, showing great promise for diagnosis and treatment.

关 键 词：nanoscale coordinationpolymer drug delivery magnetic resonanceimaging stimuli-responsivenanocarriers 

分 类 号：U666.7[交通运输工程—船舶及航道工程] TE357.46[交通运输工程—船舶与海洋工程]