Abstract

Magnetic resonance imaging (MRI) is a powerful tool for non-invasive, high-resolution three-dimensional medical imaging of anatomical structures such as organs and tissues. The use of contrast agents based on gadolinium chelates started in 1988 to improve the quality of the image, since researchers and industry focused their attention on the development of more efficient and stable structures. This review is about the state of the art of MRI contrast agents based on cyclodextrin scaffolds. Chemical engineering strategies are herein reported including host–guest inclusion complexation and covalent linkages. It also offers descriptions of the MRI properties and in vitro and in vivo biomedical applications of these emerging macrostructures. It highlights that these supramolecular associations can improve the image contrast, the sensitivity, and the efficiency of MRI diagnosis by targeting cancer tumors and other diseases with success proving the great potential of this natural macrocycle.

Highlights

  • Magnetic resonance imaging (MRI) is a powerful tool for noninvasive, high-resolution three-dimensional medical imaging of anatomical structures such as organs and tissues

  • We focused our report on cyclodextrins, a scaffold selected because it can be highly chemically modi able

  • From a pioneering work mainly managed by an Italian group based on the use of cyclodextrin scaffold led to fundamental results allowing us to better understand the mechanism and the interactions which could in uence positively the efficiency of the paramagnetic chelates

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Summary

Introduction

Magnetic resonance imaging (MRI) is a powerful tool for noninvasive, high-resolution three-dimensional medical imaging of anatomical structures such as organs and tissues. The large size and high molecular weight of the paramagnetic chelate are determinant parameters to positively affect the rotational correlation time (sr) and the residence time of water molecules (sm) in the sphere of coordination of the metal.[9,10,11,12,13,14] Slower rotation (an increase of sr) and faster exchange rate kex (decrease of sm, kex 1⁄4 1/sm) improve the relaxivity. The challenge in the MRI research eld is to reach a potent CA that can ll successfully parameters such as high relaxivity value to reach good contrast imaging with strong coordinating ligands to avoid the release of free Gd(III) into the bloodstream and, high sensitivity to extend the applications to the detection of low concentrated biological targets, typically 10À9 to 10À13 mol gÀ1 in cell tissue with stable relaxivity in clinical and animal imaging experimental conditions. More and more sophisticated supramolecular designs are currently reported to target and visualize cancer tumors and other diseases with success proving the great potential of this natural macrocycle

Noncovalent host–guest inclusion complexes
H H BOM H BOM
Cyclodextrins covalently linked to contrast agents
Acetate and iminoacetate ligands
Polymers of cyclodextrins
Polyrotaxanes
Dendrimers
Findings
Conclusions and outlook
Full Text
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