A Near-Infrared-II Polymer with Tandem Fluorophores Demonstrates Superior Biodegradability for Simultaneous Drug Tracking and Treatment Efficacy Feedback

作者：Wei, Dengshuai; Yu, Yingjie; Huang, Yun; Jiang, Yuming; Zhao, Yao; Nie, Zongxiu; Wang, Fuyi; Ma, Wen; Yu, Zhiqiang; Huang, Yuanyu; Zhang, Xiao-Dong; Liu, Zhao-Qian; Zhang, Xingcai; Xiao, Haihua^*

来源：ACS Nano, 2021, 15(3): 5428-5438.

DOI：10.1021/acsnano.1c00076

• biodegradable
• NIR-II polymers
• drug tracking
• apoptosis imaging
• targeted therapy

NIR-II (1000-1700 nm) fluorescence imaging is continually attracting strong research interest. However, current NIR-II imaging materials are limited to small molecules with fast blood clearance and inorganic nanomaterials and organic conjugated polymers of poor biodegradability and low biocompatibility. Here, we report a highly biodegradable polyester carrying tandem NIR-II fluorophores as a promising alternative. The polymer encapsulated a platinum intercalator (56MESS, (5,6-dimethyl-1,10-phenanthroline) (1S,2S-diamino-cyclohexane) platinum(II)) and was conjugated with both a cell-targeting RGD peptide and a caspase-3 cleavable peptide probe to form nanoparticles for simultaneous NIR-II and apoptosis imaging. In vitro, the nanoparticles were approximately 4-1000- and 1.5-10-fold more potent than cisplatin and 56MESS, respectively. Moreover, in vivo, they significantly inhibited tumor growth on a multidrug-resistant patient-derived mouse model (PDXMDR). Finally, through label-free laser desorption-ionization mass spectrometry imaging (MALDI-MSI), in situ 56MESS release in the deeper tumors was observed. This work highlighted the use of biodegradable NIR-II polymers for monitoring drugs in vivo and therapeutic effect feedback in real-time.

• 单位
  1; 南方医科大学; 北京理工大学; 中国科学院; 中国科学院研究生院; 天津大学