177 Lu Radiolabelled AIE Dots for Multimodal Imaging Guided Photothermal/Radiopharmaceutical Tumor Therapy.

Aggregation-induced emission luminogens (AIEgens) in the second near-infrared region (NIR-II,1000-1700 nm) have shown tremendous potential as theragnostic probe for tumor multimodal diagnostic imaging and combined treatment owing to their programmable optical, structural and functional properties. Herein, we presented a radionuclide 177 Lu-labeled AIEgen, 177 Lu-2TT-oC6B dots, for NIR-II fluorescence and SPECT/CT imaging-guided tumor photothermal and radiopharmaceutical therapy. Intriguingly, 177 Lu-2TT-oC6B self-assembled into 10 nm dots, exhibited high NIR-II fluorescence quantum yield (QY, 1.34 %) and unprecedented photothermal conversion efficiency (PCE, 70.3 %) in vitro, furtherly performed extremely long blood circulation (T1/2 =52.4 h), persistent tumor accumulation and retention in tumor (NIR-II SNR=5.56; SPECT SNR=36.59) via intravenous administration in vivo. Furthermore, upon NIR light activation and 177 Lu irradiation, 177 Lu-2TT-oC6B demonstrated great application potential in synergistic photothermal/radiopharmaceutical tumor therapy.

Aggregation-induced Emission Based Fluorogens for Mitochondria-targeted Tumor Imaging and Theranostics.

Occurrence and development of cancer are multifactorial and multistep processes which involve complicated cellular signaling pathways. Mitochondria, as the energy producer in cells, play key roles in tumor cell growth and division. Since mitochondria of tumor cells have a more negative membrane potential than those of normal cells, several fluorescent imaging probes have been developed for mitochondria-targeted imaging and photodynamic therapy. Conventional fluorescent dyes suffer from aggregation-caused quenching effect, while novel aggregation-induced emission (AIE) probes are ideal candidates for biomedical applications due to their large stokes shift, strong photo-bleaching resistance, and high quantum yield. This review aims to introduce the recent advances in the design and application of mitochondria-targeted AIE probes. The comprehensive review focuses on the structure-property relationship of these imaging probes, expecting to inspire the development of more practical and versatile AIE fluorogens (AIEgens) as tumor imaging and therapy agents for preclinical and clinical use.