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Dendritic MRI contrast agents: An efficient prelabeling approach based on CuAAC

AuthorsFernández-Trillo, Francisco; Pacheco-Torres, Jesús; Correa, Juan; Ballesteros, Paloma ; López-Larrubia, Pilar ; Cerdán, Sebastián ; Riguera, Ricardo; Fernandez-Megia, Eduardo
Issue Date2011
PublisherAmerican Chemical Society
CitationBiomacromolecules 12(8): 2902-2907 (2011)
AbstractThe Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) allows the efficient and complete functionalization of dendrimers with preformed Gd chelates (prelabeling) to give monodisperse macromolecular contrast agents (CAs) for magnetic resonance imaging (MRI). This monodispersity contrasts with the typical distribution of materials obtained by classical routes and facilitates the characterization and quality control demanded for clinical applications. The potential of a new family of PEG-dendritic CA based on a gallic acid-triethylene glycol (GATG) core functionalized with up to 27 Gd complexes has been explored in vitro and in vivo, showing contrast enhancements similar to those of Gadomer-17, which reveals them to be a promising platform for the development of CA for MRI. © 2011 American Chemical Society.
Identifiersdoi: 10.1021/bm2004466
issn: 1525-7797
e-issn: 1526-4602
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