Peptide-based soft hydrogels modified with gadolinium complexes as MRI contrast agents

Enrico Gallo, Carlo Diaferia, Enza Di Gregorio, Giancarlo Morelli, Eliana Gianolio, Antonella Accardo

Research output: Contribution to journalArticlepeer-review

Abstract

Poly-aromatic peptide sequences are able to self-assemble into a variety of supramolecular aggregates such as fibers, hydrogels, and tree-like multi-branched nanostructures. Due to their biocompatible nature, these peptide nanostructures have been proposed for several applications in biology and nanomedicine (tissue engineering, drug delivery, bioimaging, and fabrication of biosensors). Here we report the synthesis, the structural characterization and the relaxometric behavior of two novel supramolecular diagnostic agents for magnetic resonance imaging (MRI) technique. These diagnostic agents are obtained for self-assembly of DTPA(Gd)-PEG8-(FY)3 or DOTA(Gd)-PEG8-(FY)3 peptide conjugates, in which the Gd-complexes are linked at the Nterminus of the PEG8-(FY)3 polymer peptide. This latter was previously found able to form selfsupporting and stable soft hydrogels at a concentration of 1.0% wt. Analogously, also DTPA(Gd)PEG8-(FY)3 and DOTA(Gd)-PEG8-(FY)3 exhibit the trend to gelificate at the same range of concentration. Moreover, the structural characterization points out that peptide (FY)3 moiety keeps its capability to arrange into β-sheet structures with an antiparallel orientation of the β-strands. The high relaxivity value of these nanostructures (~12 mM−1·s−1 at 20 MHz) and the very low in vitro cytotoxicity suggest their potential application as supramolecular diagnostic agents for MRI.

Original languageEnglish
Article number19
JournalPharmaceuticals
Volume13
Issue number2
DOIs
Publication statusPublished - Feb 2020

Keywords

  • Diagnostic agents
  • Hydrogels
  • In vitro cytotoxicity
  • MRI contrast agents
  • Peptide conjugates

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science

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