Development of sup(177)Lu-DOTA-dendrimer and determination of its effect on metal and ion levels in tumor tissue
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Cancer Biotherapy and Radiopharmaceuticals
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Dendrimers are synthetic nanomolecules with well-defined chemical structures. Different strategies have been
used for radiolabeling dendrimers with different radioisotopes. In this study, the aim was to conjugate dendrimers with 177Lu, to observe the in vivo behavior of the labeled compound and to measure the elementary
changes in tumor tissue that could be caused by ionizing radiation. PAMAM G4 dendrimers conjugated with
DOTA were labeled with 177Lu. The radiolabeled compound was characterized and its stability was evaluated
by reverse phase high performance liquid chromatography. Radiolabeling yield was >98% and stable for 24
hours. Biodistribution studies of 177Lu-DOTA-dendrimers in C57BL/6 melanoma-bearing mice showed blood
clearance with hepatic and renal depuration and tumor uptake. The concentrations of Br, Ca, Cl, Fe, K, Mg, Na,
Rb, S, and Zn were determined in tumor tissues of C57BL/6 mice treated with 177Lu-DOTA-dendrimers and in
untreated mice. The results showed decreased concentrations of Br (62%), Ca (24%), Cl (51%), K (12%) and
Na (60%) and increased concentrations of Fe (8%), Mg (28%), Rb (100%), S (6%) and Zn (4%) in tumor tissues
of mice treated with 177Lu-DOTA-dendrimers. These data may be useful to evaluate changes in tumor tissues as
indicators of damage that could be caused by ionizing radiation.
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KOVACS, LUCIANA; TASSANO, MARCOS; CABRERA, MIREL; ZAMBONI, CIBELE B.; FERNANDEZ, MARCELO; ANJOS, ROBERTO M.; CABRAL, PABLO. Development of sup(177)Lu-DOTA-dendrimer and determination of its effect on metal and ion levels in tumor tissue. Cancer Biotherapy and Radiopharmaceuticals, v. 30, n. 10, p. 405-409, 2015. DOI: 10.1089/cbr.2014.1675. Disponível em: http://repositorio.ipen.br/handle/123456789/25430. Acesso em: 30 Dec 2025.
Esta referência é gerada automaticamente de acordo com as normas do estilo IPEN/SP (ABNT NBR 6023) e recomenda-se uma verificação final e ajustes caso necessário.