Hypoxia-activatable nano-prodrug for fluorescently tracking drug release in mice


Chemotherapy is one of the commonly used methods to treat various types of cancers in clinic by virtue of its high efficiency and universality. However, strong side effects and low concentration of conventional drugs at the tumor site have always been important factors that plague the chemotherapy effects of patients, further precluding their practical applications. Thereof, to solve the above dilemma, by integration of anticancer drug (nitrogen mustard, NM) into an NIR fluorophore (a dicyanoisophorone derivative), an intelligent prodrug NIR-NM was developed via molecular engineering strategy. Prodrug NIR-NM stimulated in hypoxia condition exhibits significantly higher toxicity to cancer cells than normal cells, essentially reducing the collateral damage to healthy cells and tissues of nitrogen mustard. More importantly, the nanoparticle prodrug FA-lip@NIR-NM showed the advantages of the high accumulation of drug at tumor site and long-circulation capacity in vivo, which endowed it the ability to track the release of the active chemotherapeutic drug and further treat solid tumors.

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This work was supported by the National Creative Research Initiative programs of the National Research Foundation of Korea (NRF), the Korean Government (MSIP) (2012R1A3A2048814), the National Natural Science Foundation of China (21421005, 21808028) and the Natural Science Foundation of Liaoning United Fund (U1608222, U1908202).

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Correspondence to Juyoung Yoon or Xiaojun Peng.

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Li, H., Yao, Q., Pu, Z. et al. Hypoxia-activatable nano-prodrug for fluorescently tracking drug release in mice. Sci. China Chem. 64, 499–508 (2021). https://doi.org/10.1007/s11426-020-9880-7

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  • NIR fluorescent probe
  • activatable
  • hypoxia
  • prodrug
  • imaging