Hypoxia-responsive polymeric nanoparticles for tumor-targeted drug delivery

Thavasyappan Thambi, V. G. Deepagan, Hong Yeol Yoon, Hwa Seung Han, Seol Hee Kim, Soyoung Son, Dong Gyu Jo, Cheol Hee Ahn, Yung Doug Suh, Kwangmeyung Kim, Ick Chan Kwon, Doo Sung Lee, Jae Hyung Park

Research output: Contribution to journalArticlepeer-review

296 Scopus citations


Hypoxia is a condition found in various intractable diseases. Here, we report self-assembled nanoparticles which can selectively release the hydrophobic agents under hypoxic conditions. For the preparation of hypoxia-responsive nanoparticles (HR-NPs), a hydrophobically modified 2-nitroimidazole derivative was conjugated to the backbone of the carboxymethyl dextran (CM-Dex). Doxorubicin (DOX), a model drug, was effectively encapsulated into the HR-NPs. The HR-NPs released DOX in a sustained manner under the normoxic condition (physiological condition), whereas the drug release rate remarkably increased under the hypoxic condition. From invitro cytotoxicity tests, it was found the DOX-loaded HR-NPs showed higher toxicity to hypoxic cells than to normoxic cells. Microscopic observation showed that the HR-NPs could effectively deliver DOX into SCC7 cells under hypoxic conditions. Invivo biodistribution study demonstrated that HR-NPs were selectively accumulated at the hypoxic tumor tissues. As consequence, drug-loaded HR-NPs exhibited high anti-tumor activity invivo. Overall, the HR-NPs might have a potential as nanocarriers for drug delivery to treat hypoxia-associated diseases.

Original languageEnglish
Pages (from-to)1735-1743
Number of pages9
Issue number5
StatePublished - Feb 2014

Bibliographical note

Funding Information:
This work was financially supported by the Converging Research Program ( 20090081876 ) and the Basic Science Research Programs ( 20100027955 & 2012012827 ) of the NRF.


  • 2-Nitroimidazole
  • Bioreduction
  • Drug delivery
  • Hypoxia
  • Nanoparticles


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