ανβ3 integrin-targeted ICG-derived probes for imaging-guided surgery and photothermal therapy of oral cancer

Indocyanine green (ICG), as the only Federal Drug Administration (FDA) approved fluorescence imaging agent, has been widely applied in clinics for near-infrared (NIR) fluorescence imaging-guided surgery and photothermal therapy of cancers. However, its lack of target specificity and poor photo and photothermal stabilities seriously restrict its wide application in clinical practice. Herein, we developed ICG-derived NIR fluorescent probes consisting of a cypate fluorophore and one or two cyclic-(arginine-glycine-aspartic acid) (cRGD) peptides that can specifically target αvβ3 integrin for accurate diagnosis and therapy of oral tumors. Probe Cy-2RGD has been demonstrated to possess bright NIR emission, great tumor targeting capability and a photothermal effect. Moreover, it could be successfully used for effective imaging-guided surgical resection as well as photothermal therapy of oral tumors. This work could provide a valuable tool for sensitive detection and accurate treatment of malignant tumors. ανβ3 integrin-targeted ICG-derived probes consisting of a cypate fluorophore and two or one cyclic-(arginine-glycine-aspartic acid) peptides was developed for NIR fluorescence imaging-guided surgery and photothermal therapy of oral cancers.