Organic NIR-II dyes with ultralong circulation persistence for image-guided delivery and therapy

Yang Li, Jianfeng Gao, Shuping Wang, Shijun Li, Xiaowen Hou, Yanna Pan, Jialu Gao, Xue Qiao, Zhiquan Tian, Deliang Chen, Hai Deng, Zixin Deng, Xuechuan Hong, Yuling Xiao*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

27 Citations (Scopus)
6 Downloads (Pure)


Nanocarriers hold great promise for the controlled release of therapeutic payloads to target organs/tissues and extended duration of anticancer agents in the bloodstream. However, limited data on their in vivo pharmacokinetics and delivery process hamper clinical applications. Here we report a series of micellar nanocarriers selfassembled from new-generation thiophenthiadiazole (TTD)-based NIR-II fluorophores HLAnP (n = 1-4) for simultaneous bioimaging and drug delivery. The NIR-II HLA4P nanocarrier displays exceptional non-fouling performance, minimal immunogenicity, ultralong blood half-life, and high tumor accumulation even with different administration routes. When used as a drug carrier, HLA4P with encapsulated doxorubicin (DOX) realized accurate tumor targeting and continuous real-time in vivo NIR-II tracking of drug delivery and therapy, showing a sustained release rate, improved therapeutic effect, and diminished cardiotoxicity as compared to free DOX. This study provides a new perspective on the design of dual-functional NIR-II fluorophores for diagnostic and therapeutic applications.

Original languageEnglish
Pages (from-to)157-169
Number of pages13
JournalJournal of Controlled Release
Early online date5 Jan 2022
Publication statusPublished - 1 Feb 2022

Bibliographical note

This work was partially supported by grants from the National Key R&D Program of China (2020YFA0908800), NSFC (82111530209, 81773674, 91959103, 81573383, 21763002), Shenzhen Science and Technology Research Grant (JCYJ20190808152019182), the Applied Basic Research Program of Wuhan Municipal Bureau of Science and Technology (2019020701011429), Hubei Province Scientific and Technical Innovation Key Project (2020BAB058), the Local Development Funds of Science and Technology Department of Tibet (XZ202102YD0033C, XZ202001YD0028C), and the Fundamental Research Funds for the Central Universities.


  • China
  • Drug delivery
  • Image-guided therapy
  • Second near-infrared window (NIR-II)
  • Self-assembly
  • Fluorescence imaging


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