Journal
PHARMACEUTICALS
Volume 13, Issue 2, Pages -Publisher
MDPI
DOI: 10.3390/ph13020019
Keywords
diagnostic agents; hydrogels; MRI contrast agents; peptide conjugates; in vitro cytotoxicity
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Funding
- Italian Minister of Education, University and Research [PRIN-2017A2KEPL]
- Regione Campania - POR Campania [B61G18000470007]
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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 N-terminus of the PEG8-(FY)3 polymer peptide. This latter was previously found able to form self-supporting 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 beta-sheet structures with an antiparallel orientation of the beta-strands. The high relaxivity value of these nanostructures (12 mM(-1)center dot s(-1) at 20 MHz) and the very low in vitro cytotoxicity suggest their potential application as supramolecular diagnostic agents for MRI.
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