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Study of fluorophore and technetium labeling of poly(amido)-amine (PAMAM) generation 4 (G4) dendrimer and its evaluation as potential molecular imaging agent in both normal and melanoma-bearing mice, are described. Dendrimers were first conjugated with FITC (fluorescein isothiocyanate). Dendrimer-FITC was then incubated with the intermediate [(99m)Tc(CO)(3)(H(2)O)(3)](+) and purified by gel filtration. Biodistribution and scintigraphy images were performed administrating (99m)Tc(CO)(3)-dendrimer-FITC to normal mice (NM) or melanoma-bearing mice (MBM). Cryostat tissue sections from MBM mice were analyzed by confocal microscopy. Radiolabeling yield of dendrimer was approx. 90%. The (99m)Tc(CO)(3)-dendrimer-FITC complex was stable for at least 24h. Biodistribution studies in NM showed blood clearance with hepatic and renal depuration. MBM showed a similar pattern of biodistribution with high tumor uptake that allowed tumor imaging. Confocal microscopy analysis showed cytoplasmic distribution of (99m)Tc(CO)(3)-dendrimer-FITC. Copyright © 2011 Elsevier Ltd. All rights reserved.


Marcos R Tassano, Paola F Audicio, Juan P Gambini, Marcelo Fernandez, Juan P Damian, Maria Moreno, Jose A Chabalgoity, Omar Alonso, Juan C Benech, Pablo Cabral. Development of 99mTc(CO)₃-dendrimer-FITC for cancer imaging. Bioorganic & medicinal chemistry letters. 2011 Sep 15;21(18):5598-601

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PMID: 21778055

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