Macromolecular ligands for gadolinium MRI contrast agents

Yang Li, Mariana Beija, Sophie Laurent, Luce Vander Elst, Robert N Muller, Hien Thi Thu Duong, Andrew B Lowe, Thomas Paul Davis, Cyrille Boyer

Research output: Contribution to journalArticleResearchpeer-review

141 Citations (Scopus)

Abstract

Macromolecular ligands for gadolinium contrast agents (CAs) were prepared via a grafting to ? strategy. Copolymers of oligoethylene glycol methyl ether acrylate (OEGA) and an activated ester monomer, pentafluorophenyl acrylate (PFPA), were synthesized and modified with the 1-(5-amino-3-aza-2- oxypentyl)-4,7,10-tris(tert-butoxycarbonylmethyl)-1,4,7,10- tetraazacyclododecane (DO3A-tBu-NH 2) chelate for the complexation of Gd 3+. The relaxivity properties of the ligated Gd 3+ agents were then studied to evaluate the effect of macromolecular architecture on their behavior as magnetic resonance imaging (MRI) CAs. Ligands made from linear and hyperbranched macromolecules showed a substantially increased relaxivity in comparison to existing commercial Gd 3+ MRI contrast agents. In contrast, star nanogel polymers exhibited a slightly lower relaxivity per Gd 3+ ion (but still substantially higher relaxivity than existing low molecular weight commercial CAs). This work shows that macromolecular ligands have the potential to serve as components of Gd MRI agents as there are enhanced effects on relaxivity, allowing for lower Gd concentrations to achieve contrast, while potentially imparting control over pharmacokinetics.
Original languageEnglish
Pages (from-to)4196 - 4204
Number of pages9
JournalMacromolecules
Volume45
Issue number10
DOIs
Publication statusPublished - 2012
Externally publishedYes

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