A feasible and biocompatible supramolecular complex self-assembled from indocyanine green (ICG) and methyl-β-cyclodextrin (Mβ-CD) was developed for targeted cancer imaging, which enhanced fluorescence-guided photothermal cancer therapy. This study confirmed that the formation of an inclusion complex of the heterocyclic ICG moiety and Mβ-CD inner cavity could result in improved tumor targetability compared with free ICG. The ICG-CD complex could be used as a bifunctional phototherapeutic agent for targeted cancer phototherapy due to the high tumor targetability of the Mβ-CD moiety and effective photothermal performance of the near-infrared (NIR) ICG moiety. Upon NIR laser irradiation, the photothermal effect exerted by the ICG-CD complex significantly enhanced the temperature at the tumor site by 56.2 °C within 5 min. Targeting HT-29 tumors using the ICG-CD complex resulted in an apparent reduction in tumor volumes over the 9 days after photothermal treatment. Moreover, no tumor recurrence or body weight loss were observed after administering a single dose of ICG-CD complex with NIR laser irradiation. Therefore, the administration of the biocompatible ICG-CD complex in combination with NIR laser treatment can be safely explored as a potential strategy for future clinical applications.
Near‐infrared (NIR) fluorescence cancer imaging with targeted NIR fluorophores holds considerable promise for accurate detection and cancer diagnosis. Among the various NIR heptamethine cyanine dyes reported previously, IR783 as a single small molecule has been widely used for tumor‐targeted imaging without the additional conjugation of targeting moieties. Despite the potential advantages of IR783, the major problems, such as its non‐specific uptake in normal tissues/organs and slow clearance, remain to be solved. A key determinant of sensitivity and detectability in tumor imaging is the improvement of the tumor‐to‐background ratio (TBR). Herein, a simple and effective supramolecular complex self‐assembled from IR783 and methyl‐β‐cyclodextrin is developed to improve tumor imaging accompanied by rapid clearance from the body. The IR783‐cyclodextrin complex allowed for rapid whole body biodistribution, which remarkably reduced non‐specific background uptake, and thus increased the TBR value within 24 h post‐injection. Therefore, this strategy is applicable in combination with many different types of carbocyanine dyes for improved tumor imaging.
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