Peptide derivatized lamellar aggregates as target-specific MRI contrast agents

The relaxivity behaviour and the structural characterization of new supramolecular aggregates (bilayer structures and micelles) obtained by combining two different amphiphilic monomers are reported. One monomer, (C18)(2)DTPAGlu-Gd, contains a very stable gadolinium complex, and the other, DSPE-PEG(2000)-CCK8, contains the bioactiv CCK8 peptide. Samples that contained only DSPE-PEG(2000)-CCK8, or up to 50% (C18)(2)DTPAGlu-Gd, aggregated as double-layer structures (lamellar aggregates) with a thickness of similar to 80-100 angstrom, as evaluated by SANS measurement and Cryo-TEM imaging. A transition to micelle formation was observed when the amount of (C18)(2)DTPAGlu-Gd in the aggregate was increased. These were rod-like micelles similar to 40 angstrom in radius and > 200 angstrom in length. The proton relaxivities for both lamellar aggregates and rod-like micelles were the same (17.2 mM(-1) s(-1)), although the values were the results of different combinations of local and global contributions. The in vitro target selectivity of aggregates that contained the CCK-8 peptide was demonstrated by using nuclear medicine techniques.