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Technetium-99m-labeled doxorubicin as an imaging probe for murine breast tumor (4T1 cell line) identification

Fernandes, Renata S ; Silva, Juliana de Oliveira ; Lopes, Savia C.A ; Chondrogiannis, Sotirios ; Rubello, Domenico ; Cardoso, Valbert N ; Oliveira, Mônica C ; Ferreira, Lucas A.M ; de Barros, André L.B

Nuclear medicine communications, 2016-03, Vol.37 (3), p.307-312 [Periódico revisado por pares]

England: Copyright Wolters Kluwer Health, Inc. All rights reserved

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Título:
Technetium-99m-labeled doxorubicin as an imaging probe for murine breast tumor (4T1 cell line) identification
Autor: Fernandes, Renata S ; Silva, Juliana de Oliveira ; Lopes, Savia C.A ; Chondrogiannis, Sotirios ; Rubello, Domenico ; Cardoso, Valbert N ; Oliveira, Mônica C ; Ferreira, Lucas A.M ; de Barros, André L.B
Assuntos: Animals ; Cell Line, Tumor ; Doxorubicin - chemistry ; Doxorubicin - pharmacokinetics ; Drug Stability ; Female ; Hydrogen-Ion Concentration ; Isotope Labeling ; Mammary Neoplasms, Experimental - diagnostic imaging ; Mammary Neoplasms, Experimental - pathology ; Mice ; Radiochemistry ; Radionuclide Imaging ; Technetium - chemistry ; Tissue Distribution
É parte de: Nuclear medicine communications, 2016-03, Vol.37 (3), p.307-312
Descrição: OBJECTIVEEarly diagnosis of malignant tumors is essential to successfully plan a radical and curative approach. In this study we describe the direct radiolabeling of doxorubicin (DOX) at physiological pH to identify murine breast tumor (4T1 cells)-bearing BALB/c mice. MATERIALS AND METHODSTechnetium-99m (Tc) DOX was prepared by adding Tc-pertechnetate to a PBS (pH 7.4) solution containing DOX in the presence of stannous chloride. Radiochemical purity and in-vitro stability were determined. The circulation time of Tc-DOX was determined by measuring blood radioactivity in healthy animals. Scintigraphic images and biodistribution studies were carried out in tumor-bearing mice at 1, 4, and 8 h after injection. RESULTSThe Tc-DOX complex showed high radiochemical purity (99.27±0.34%) and in-vitro stability until 8 h. Tc-DOX levels in blood declined in a biphasic manner, with an α half-life of 4.5 min and a β half-life of 277.2 min. High uptake was achieved in kidneys, liver, and spleen, because of the drug elimination routes. Moreover, tumor uptake was higher than that of control tissue, resulting in high tumor-to-muscle ratios. CONCLUSIONDOX was successfully labeled with Tc-pertechnetate and showed high stability. Biodistribution and scintigraphic studies indicated high tumor-to-muscle ratios in breast tumor-bearing BALB/c mice. These results suggested the feasibility of Tc-DOX as a functional agent in tumor diagnosis.
Editor: England: Copyright Wolters Kluwer Health, Inc. All rights reserved
Idioma: Inglês

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Technetium-99m-labeled doxorubicin as an imaging probe for murine breast tumor (4T1 cell line) identification

Fernandes, Renata S ; Silva, Juliana de Oliveira ; Lopes, Savia C.A ; Chondrogiannis, Sotirios ; Rubello, Domenico ; Cardoso, Valbert N ; Oliveira, Mônica C ; Ferreira, Lucas A.M ; de Barros, André L.B

England: Copyright Wolters Kluwer Health, Inc. All rights reserved

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