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

Zhang, Songbai; Lloveras, Vega; Pulido, Daniel; Liko, Flonja; Pinto, Luiz F.; Albericio, Fernando; Royo, Miriam; Vidal-Gancedo, José

doi:10.3390/pharmaceutics12080772

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

^1,†

^1,†

^2,3,4

and

^1,*

Institut de Ciència de Materials de Barcelona (ICMAB-CSIC) and CIBER-BBN, Campus Universitari de Bellaterra, Bellaterra, 08193 Barcelona, Spain

Institut de Química Avançada de Catalunya (IQAC-CSIC) and CIBER-BBN c/ Jordi Girona 18–26, 08034 Barcelona, Spain

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

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. View Full-Text

Keywords: 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

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

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