College of Chemistry, Key Laboratory of Functional Polymer Materials (Ministry of Education), State Key Laboratory of Elemento-Organic Chemistry, Tianjin Key Laboratory of Biosensing and Molecular Recognition, Nankai University, Tianjin 300071, China.
Key Laboratory of Radiopharmacokinetics for Innovative Drugs, Chinese Academy of Medical Sciences, Institute of Radiation Medicine Chinese Academy of Medical Science & Peking Union Medical College, Tianjin 300192, China.
Theranostics. 2022 Jan 1;12(1):396-409. doi: 10.7150/thno.67036. eCollection 2022.
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. 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 and . 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 and . 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.
基于有机小分子染料的光热剂 (PTAs) 作为一种有前途的成像和光热治疗 (PTT) 治疗策略而出现。然而,疏水性、光降解和低信噪比阻碍了它们从实验室向临床的转化。在这项研究中,通过响应性大环主体制备了一种新型的刺激响应超分子 PTT 制剂,以克服有机小分子 PTA 的这些障碍。合成磺化杯[4]芳烃 (SAC4A) 作为缺氧响应性大环主体。以 IR780 为例,通过研磨法构建了超分子纳米制剂 IR780@SAC4A,并对其溶解度、光稳定性和光热转换进行了评价。进一步评价了 IR780@SAC4A 的缺氧肿瘤选择性成像和超分子 PTT。IR780@SAC4A 能够显著提高 IR780 的溶解度、光稳定性和光热转换效率,使这种超分子制剂具有良好的成像指导 PTT 疗效。该研究表明,超分子 PTT 策略是一种很有前途的癌症治疗方法。此外,这种超分子方法适用于构建各种超分子 PTA,为扩展智能 PTT 制剂开辟了一条通用途径。
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