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

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 serie...

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Veröffentlicht in:Journal of controlled release 2022-02, Vol.342, p.157-169
Hauptverfasser: Li, Yang, Gao, Jianfeng, Wang, Shuping, Li, Shijun, Hou, Xiaowen, Pan, Yanna, Gao, Jialu, Qiao, Xue, Tian, Zhiquan, Chen, Deliang, Deng, Hai, Deng, Zixin, Hong, Xuechuan, Xiao, Yuling
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Sprache:eng
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Zusammenfassung: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 self-assembled 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. An ultralow fouling NIR-II probe HLA4P self-assembled into micelles with long-circulation persistence and ultrahigh signal-background ratio for routine preoperative tumor assessment and trackable drug delivery. [Display omitted] •A new TTD-based NIR-II dye (HLA4P) with a high fluorescence QY, exceptional nonfouling performance and low immunogenicity.•HLA4P exhibited ultralong blood circulation, super-contrast ratio and long tumor retention by various injection routes.•HLA4P could be simultaneously used for long-term in vivo NIR-II tracking of drug delivery and therapy.•HLA4P@DOX showed sustained DOX release behavior, enhanced therapeutic effect and diminished toxicity.
ISSN:0168-3659
1873-4995
DOI:10.1016/j.jconrel.2022.01.005