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

Chem Asian J. 2023 Dec 1;18(23):e202300847. doi: 10.1002/asia.202300847. Epub 2023 Nov 2.

Abstract

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.

Keywords: aggregation-induced emission (AIE); multi-modality imaging; single-photon emission computed tomography (SPECT); the second near-infrared fluorescence (NIR-II FL); theragnostic.

MeSH terms

  • Humans
  • Multimodal Imaging
  • Nanoparticles* / chemistry
  • Neoplasms* / diagnostic imaging
  • Neoplasms* / drug therapy
  • Optical Imaging / methods
  • Photothermal Therapy
  • Radiopharmaceuticals / pharmacology

Substances

  • Radiopharmaceuticals