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Volume 12
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Article

Radical Dendrimers Based on Biocompatible Oligoethylene Glycol Dendrimers as Contrast Agents for MRI

by
Songbai Zhang
1,†,
Vega Lloveras
1,†,
Daniel Pulido
2,
Flonja Liko
1,
Luiz F. Pinto
1,
Fernando Albericio
2,3,4,
Miriam Royo
2 and
José Vidal-Gancedo
1,*
1
Institut de Ciència de Materials de Barcelona (ICMAB-CSIC) and CIBER-BBN, Campus Universitari de Bellaterra, Bellaterra, 08193 Barcelona, Spain
2
Institut de Química Avançada de Catalunya (IQAC-CSIC) and CIBER-BBN c/ Jordi Girona 18–26, 08034 Barcelona, Spain
3
Department of Inorganic and Organic Chemistry, University of Barcelona, 08028 Barcelona, Spain
4
School of Chemistry and Physics, University of KwaZulu-Natal, Durban 4041, South Africa
*
Author to whom correspondence should be addressed.
†
These authors contributed equally to the work.
Pharmaceutics 2020, 12(8), 772; https://doi.org/10.3390/pharmaceutics12080772
Submission received: 12 June 2020 / Revised: 23 July 2020 / Accepted: 3 August 2020 / Published: 14 August 2020
(This article belongs to the Special Issue Dendrimers and Dendritic Materials against Infectious Diseases)
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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 r1 relaxivity value (3.4 mM−1s−1) in comparison to gadolinium-diethylenetriamine pentaacetic acid (Gd-DTPA) used in clinics (3.2 mM−1s−1, 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.
Keywords: contrast agent; magnetic resonance imaging (MRI); organic radicals; PROXYL; OEG dendrimers; radical dendrimers; relaxivity; Gd-DTPA; infectious diseases contrast agent; magnetic resonance imaging (MRI); organic radicals; PROXYL; OEG dendrimers; radical dendrimers; relaxivity; Gd-DTPA; infectious diseases
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MDPI and ACS Style

Zhang, S.; Lloveras, V.; Pulido, D.; Liko, F.; Pinto, L.F.; Albericio, F.; Royo, M.; Vidal-Gancedo, J. Radical Dendrimers Based on Biocompatible Oligoethylene Glycol Dendrimers as Contrast Agents for MRI. Pharmaceutics 2020, 12, 772. https://doi.org/10.3390/pharmaceutics12080772

AMA Style

Zhang S, Lloveras V, Pulido D, Liko F, Pinto LF, Albericio F, Royo M, Vidal-Gancedo J. Radical Dendrimers Based on Biocompatible Oligoethylene Glycol Dendrimers as Contrast Agents for MRI. Pharmaceutics. 2020; 12(8):772. https://doi.org/10.3390/pharmaceutics12080772

Chicago/Turabian Style

Zhang, Songbai, Vega Lloveras, Daniel Pulido, Flonja Liko, Luiz F. Pinto, Fernando Albericio, Miriam Royo, and José Vidal-Gancedo. 2020. "Radical Dendrimers Based on Biocompatible Oligoethylene Glycol Dendrimers as Contrast Agents for MRI" Pharmaceutics 12, no. 8: 772. https://doi.org/10.3390/pharmaceutics12080772

APA Style

Zhang, S., Lloveras, V., Pulido, D., Liko, F., Pinto, L. F., Albericio, F., Royo, M., & Vidal-Gancedo, J. (2020). Radical Dendrimers Based on Biocompatible Oligoethylene Glycol Dendrimers as Contrast Agents for MRI. Pharmaceutics, 12(8), 772. https://doi.org/10.3390/pharmaceutics12080772

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