A tumour-selective cascade activatable self-detained system for drug delivery and cancer imaging

Hong Wei An, Li Li Li, Yi Wang, Ziqi Wang, Dayong Hou, Yao Xin Lin, Sheng Lin Qiao, Man Di Wang, Chao Yang, Yong Cong, Yang Ma, Xiao Xiao Zhao, Qian Cai, Wen Ting Chen, Chu Qi Lu, Wanhai Xu, Hao Wang, Yuliang Zhao

Research output: Contribution to journalArticlepeer-review

118 Scopus citations


Achieving the activation of drugs within cellular systems may provide targeted therapies. Here we construct a tumour-selective cascade activatable self-detained system (TCASS) and incorporate imaging probes and therapeutics. We show in different mouse models that the TCASS system accumulates in solid tumours. The molecules show enhanced accumulation in tumour regions via the effect of recognition induced self-assembly. Analysis of the molecular penetration in tumour tissue shows that in vivo self-assembly increases the penetration capability compared to typical soft or hard nanomaterials. Importantly, the in vivo self-assembled molecules exhibit a comparable clearance pathway to that of small molecules, which are excreted from organs of the reticuloendothelial system (liver and kidney), while are relatively slowly eliminated from tumour tissues. Finally, this system, combined with the NIR probe, shows high specificity and sensitivity for detecting bladder cancer in isolated intact patient bladders.

Original languageEnglish (US)
Article number4861
JournalNature Communications
Issue number1
StatePublished - Dec 1 2019

ASJC Scopus subject areas

  • Chemistry(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Physics and Astronomy(all)


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