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Radical Dendrimers Based on Biocompatible Oligoethylene Glycol Dendrimers as Contrast Agents for MRI.
- Source :
-
Pharmaceutics [Pharmaceutics] 2020 Aug 14; Vol. 12 (8). Date of Electronic Publication: 2020 Aug 14. - Publication Year :
- 2020
-
Abstract
- Finding alternatives to gadolinium (Gd)-based contrast agents (CA) with the same or even better paramagnetic properties is crucial to overcome their established toxicity. Herein we describe the synthesis and characterization of entirely organic metal-free paramagnetic macromolecules based on biocompatible oligoethylene glycol dendrimers fully functionalized with 5 and 20 organic radicals (OEG Gn-PROXYL ( n = 0, 1) radical dendrimers) with the aim to be used as magnetic resonance imaging (MRI) contrast agents. Conferring high water solubility on such systems is often a concern, especially in large generation dendrimers. Our approach to overcome such an issue in this study is by synthesizing dendrimers with highly water-soluble branches themselves. In this work, we show that the highly water-soluble OEG Gn-PROXYL ( n = 0, 1) radical dendrimers obtained showed properties that convert them in good candidates to be studied as contrast agents for MRI applications like diagnosis and follow-up of infectious diseases, among others. Importantly, with the first generation radical dendrimer, a similar r <subscript>1</subscript> relaxivity value (3.4 mM <superscript>-1</superscript> s <superscript>-1</superscript> ) in comparison to gadolinium-diethylenetriamine pentaacetic acid (Gd-DTPA) used in clinics (3.2 mM <superscript>-1</superscript> s <superscript>-1</superscript> , r.t. 7T) has been obtained, and it has been shown to not be cytotoxic, avoiding the toxicity risks associated with the unwanted accumulation of Gd in the body.
Details
- Language :
- English
- ISSN :
- 1999-4923
- Volume :
- 12
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 32823903
- Full Text :
- https://doi.org/10.3390/pharmaceutics12080772