Facile Supramolecular Approach to Nucleic-Acid-Driven Activatable Nanotheranostics That Overcome Drawbacks of Photodynamic Therapy

Xingshu Li, Sungsook Yu, Dayoung Lee, Gyoungmi Kim, Buhyun Lee, Yejin Cho, Bi Yuan Zheng, Mei Rong Ke, Jian Dong Huang, Ki Taek Nam, Xiaoyuan Chen, Juyoung Yoon

Research output: Contribution to journalArticlepeer-review

138 Scopus citations


Supramolecular chemistry provides a "bottom-up" method to fabricate nanostructures for biomedical applications. Herein, we report a facile strategy to directly assemble a phthalocyanine photosensitizer (PcS) with an anticancer drug mitoxantrone (MA) to form uniform nanostructures (PcS-MA), which not only display nanoscale optical properties but also have the capability of undergoing nucleic-acid-responsive disassembly. These supramolecular assemblies possess activatable fluorescence emission and singlet oxygen generation associated with the formation of free PcS, mild photothermal heating, and a concomitant chemotherapeutic effect associated with the formation of free MA. In vivo evaluations indicate that PcS-MA nanostructures have a high level of accumulation in tumor tissues, are capable of being used for cancer imaging, and have significantly improved anticancer effect compared to that of PcS. This study demonstrates an attractive strategy for overcoming the limitations of photodynamic cancer therapy.

Original languageEnglish
Pages (from-to)681-688
Number of pages8
JournalACS Nano
Issue number1
StatePublished - 23 Jan 2018

Bibliographical note

Funding Information:
J.-D.H. thanks National Natural Science Foundation of China (Grant Nos. 21473033, 21301031, 21172037). J.Y. thanks the National Research Foundation of Korea (NRF), which was funded by the Korea government (MSIP) (No. 2012R1A3A2048814). K.T.N. thanks the Korea Mouse Phenotyping Project (NRF-2016M3A9D5A01952416) of the National Research Foundation, and the Brain Korea 21 PLUS Project for Medical Science, Yonsei University. X.C. thanks the Intramural Research Program (IRP), National Institute of Biomedical Imaging and Bioengineering (NIBIB), and National Institutes of Health (NIH).

Publisher Copyright:
© 2017 American Chemical Society.


  • activatable
  • nanotheranostics
  • nucleic-acid-responsive disassembly
  • photodynamic therapy
  • supramolecular assembly


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