Journal
THERANOSTICS
Volume 12, Issue 1, Pages 396-409Publisher
IVYSPRING INT PUBL
DOI: 10.7150/thno.67036
Keywords
supramolecular chemistry; photothermal therapy; hypoxia; calixarene; IR780
Categories
Funding
- NSFC [U20A20259, 31961143004, 52073306]
- NCC Fund [NCC2020FH04]
- Fundamental Research Funds for the Central Universities
- Nonprofit Central Research Institute Fund of Chinese Academy of Medical Sciences [2018PT35031]
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This study presents a novel supramolecular photothermal agent (PTA) prepared using a stimuli-responsive macrocyclic host, which overcomes the challenges of hydrophobicity, photodegradation, and low signal-to-noise ratio faced by organic small-molecule PTAs. The supramolecular PTA demonstrates enhanced solubility, photostability, and photothermal conversion, and exhibits promising imaging-guided photothermal therapy efficacy both in vitro and in vivo.
Photothermal agents (PTAs) based on organic small-molecule dyes emerge as promising theranostic strategy in imaging and photothermal therapy (PTT). However, hydrophobicity, photodegradation, and low signal-to-noise ratio impede their transformation from bench to bedside. In this study, a novel supramolecular PTT formulation by a stimuli-responsive macrocyclic host is prepared to overcome these obstacles of organic small-molecule PTAs. Methods: Sulfonated azocalix[4]arene (SAC4A) was synthesized as a hypoxia-responsive macrocyclic host. Taking IR780 as an example, the supramolecular nanoformulation IR780@SAC4A was constructed by grinding method, and its solubility, photostability, and photothermal conversion were evaluated. The hypoxia tumor-selective imaging and supramolecular PTT of IR780@SAC4A were further evaluated in vitro and in vivo. Results: IR780@SAC4A is capable of enhancing the solubility, photostability, and photothermal conversion of IR780 significantly, which achieve this supramolecular formulation with good imaging-guided PTT efficacy in vitro and in vivo. Conclusions: This study demonstrates that the supramolecular PTT strategy is a promising cancer theranostic method. Moreover, this supramolecular approach is applicative to construct kinds of supramolecular PTAs, opening a general avenue for extending smart PTT formulations.
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