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

Author:

Huang Haoying1,Yu Kaiwu2,Husamelden Elkawad1,Zhang Hong13,Mao Zhengwei3,Liu Shunjie4,Zhang Qinghua2,Tian Mei1,Zhang Haoke1,He Qinggang2ORCID

Affiliation:

1. Department of Nuclear Medicine and PET Center the Second Hospital of Zhejiang University School of Medicine Hangzhou 310009 P. R. China

2. College of Chemical and Biological Engineering Zhejiang University Hangzhou 310058 P. R. China

3. MOE Key Laboratory of Macromolecular Synthesis and Functionalization Department of Polymer Science and Engineering Zhejiang University Hangzhou 310027 P.R. China

4. Key Laboratory of Polymer Ecomaterial Changchun Institute of Applied Chemistry Chinese Academy of Sciences Changchun 130022 P.R. China

Abstract

AbstractAggregation‐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 177Lu‐labeled AIEgen, 177Lu‐2TT‐oC6B dots, for NIR‐II fluorescence and SPECT/CT imaging‐guided tumor photothermal and radiopharmaceutical therapy. Intriguingly, 177Lu‐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 177Lu irradiation, 177Lu‐2TT‐oC6B demonstrated great application potential in synergistic photothermal/radiopharmaceutical tumor therapy.

Funder

National Natural Science Foundation of China

Fundamental Research Funds for the Central Universities

Publisher

Wiley

Subject

General Chemistry,Biochemistry,Organic Chemistry

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