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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)