Radiolabeled AIE Probes as Dual‐modality Imaging Agents for PET/NIR‐II Fluorescence‐Guided Photothermal Therapy

A NIR-II AIEgen was encapsulated with amphiphilic polymers to form water-soluble nanoparticles, which were radiolabeled with ⁶⁸Ga radionuclides for bimodal PET/fluorescence imaging-guided breast tumor photothermal. With strong photothermal conversion ability and highly efficient tumor accumulation of the prepared AIE NPs, massive destruction of tumor cells was demonstrated in vitro and in vivo.

Abstract

Breast cancer has become a huge burden with continued rise of incidence and death rate worldwide. Various methods for diagnosis and therapy of breast cancer have met the challenges of lack of complete information about the tumor location and limited therapy efficacy. Although aggregation-induced emission luminogens (AIEgens) have shown great promise for various cancer treatment applications, they may be incompetent for deep-seated tumor diagnosis due to the limited penetration depth. Herein, we designed and prepared a radiolabeled AIEgen-based organic photothermal agent for bimodal PET/fluorescence imaging-guided breast tumor photothermal therapy. The prepared multifunctional nanoparticles (⁶⁸Ga-TPA-TTINC NPs) with NIR-II fluorescence, gamma irradiation and photothermal conversion property could be efficiently taken up by tumor cells and induce reactive oxygen species burst in vitro, further boosting the photothermal treatment of tumor in vivo. More importantly, the nanoprobe could target and clearly visualize 4T1 tumor xenografts through PET and NIR-II fluorescence imaging with high tumor/muscle ratio up to 4.8, which provides a promising tool and solution for breast tumor theranostics.

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