Macromolecular Imaging Agents Containing Lanthanides: Can Conceptual Promise Lead to Clinical Potential?

摘要: Macromolecular magnetic resonance imaging (MRI) contrast agents are increasingly being used to improve the resolution of this noninvasive diagnostic technique. All clinically-approved T1 small molecule chelates gadolinium [Gd(III)] that affect bound water proton relaxivity. Both size and monomeric nature these ultimately limits image enhancement can be achieved for both pharmacokinetic/biodistribution reasons. The multimeric macromolecules, such as polymers, dendrimers, noncovalent complexes with proteins, have been shown significantly increase due their large ability incorporate multiple Gd(III) chlelation sites. Also, macromolecular advantageous they designed nontoxic, hydrophilic, easily purified, aggregation-resistant, controllable three-dimensional structure housing lanthanide chelation For reasons, diagnostics relaxivity protons within targeted tissues thus many applications. FDA approval a agent consists reversible, non-covalent coupling chelate serum albumin blood pool (marketed under trade names Vasovist Ablivar) proved one first capitalize on benefits from association in humans. However, much research development is necessary optimize safety unique vivo use potential clinical development. To end, recent work field polymer, dendrimer, complex-based reviewed herein future outlook discussed.