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Table 4 Representative studies evaluating 177Lu-labeled nanoparticles in preclinical cancer models

From: Radiolabeled nanomaterials for biomedical applications: radiopharmacy in the era of nanotechnology

177Lu-labeled NPs NPs/chelate Experimental conditions t (min)/T(ºC)/pH Radiochemical yield (%) Evaluated applications References
[177Lu]Lu-DNAuNPs-folate-bombesin AuNPs/DOTA 30 min/90 °C/pH 5 Plasmonic–photothermal therapy, optical imaging, and radionuclide therapy by targeting both GRPr and FR overexpressed on breast cancer. In vitro results Mendoza-Nava et al. 2017)
[177Lu]Lu-AuNPs-PEG-Trastuzumab AuNPs/DOTA 30 min/80 °C/pH 4.5 Radionuclide therapy by targeting HER2 overexpressed on breast cancer. In vitro and in vivo results Cai et al. 2017)
[177Lu]Lu-AuNPs-RGD-NLS-Aptamer AuNPs/DOTA 30 min/90 °C/pH 5 Antiangiogenic properties, photothermal therapy, and radionuclide therapy by targeting both α(v)β(3) integrin and VEGF overexpressed in the tumor neovasculature In vitro and in vivo results using rat glioma cell lines González-Ruíz et al. 2018; González-Ruíz et al. 2017)
[177Lu]Lu-CNS-cNGR CNS/DOTA 20 min/80 °C/pH 4 80 ± 2% Radionuclide therapy by targeting aminopeptidase N receptors overexpressed on tumor angiogenic blood vessels and tumor cells. In vitro and in vivo results using melanoma cell lines Vats et al. 2018)
[177Lu]Lu-DN(PTX)-Bombesin DN/DOTA 60 min/37 °C/pH 5 Chemotherapy, nuclear imaging, and radionuclide therapy by GRPr overexpressed on breast cancer. In vitro and in vivo results Gibbens-Bandala et al. 2019)
[177Lu]Lu2O3-HSA Lu2O3/chelate-free 30 min/25 °C 84–87% Radionuclide therapy targeting tumor vasculature. In vitro and in vivo results using melanoma cell lines Chakravarty et al. 2020)
[177Lu]Lu-Cubosome(DOX) Cubosome/DOTAGA 30 min/95 °C/pH 5  > 99% Chemotherapy and radionuclide therapy. In vitro results using human-derived HeLa cancer cells Cytryniak et al. 2020)
[177Lu]Lu2O3-iPSMA Lu2O3/chelate-free Neutron activation at a neutron flux of 1 × 1013 n·s−1.cm−2 for 20 h Optical imaging and radionuclide therapy by targeting prostate-specific membrane antigen (PSMA). In vitro results using PSMA-positive hepatocellular carcinoma cell lines Ancira-Cortez et al. 2020)
[177Lu]Lu@AuNCs AuNCs/glutathione 20 min/37 °C 901% Radio-immunotherapy of cancer. In vitro and in vivo results using breast and colon cancer cell lines Pei et al. 2021b)
[177Lu]Lu-PCN-PEG nMOFs/porphyrin 30 min/37 °C 94% Radionuclide therapy. In vitro and in vivo results using breast cancer cell lines Tao et al. 2021)
[177Lu]Lu-CH CH/chelate-free 30 min/25 °C/pH 5 Radionuclide therapy. In vitro results using epithelial lung cancer cell lines Gaikwad et al. 2021)
[177Lu]Lu-GML (glucose-modified liposomes) Liposomes/chelate-free 30 min/25 °C/pH 5.5 97% Radionuclide therapy by targeting glucose transporters on the tumor vascular endothelium and tumor cells. In vivo results using colon cancer cell lines Cvjetinović et al. 2021)
[177Lu]Lu-CNC-V CNC/DOTA 60 min/100 °C/pH 4 74 ± 2% Chemotherapy and radionuclide therapy by targeting the serine/threonine protein kinase BRAF in melanoma. In vitro and in vivo results using a lung metastatic melanoma model Imlimthan et al. 2021)