Peptide containing vesicles as selective nanocarriers for therapeutics and diagnostics.

One strategy to achieve cancer-targeted drug delivery is the labeling of the supramol. aggregates with bioactive markers such as peptides. Through design, synthesis, and physicochem. characterization, target-specific supramol. aggregates, contg. a surface-exposed bioactive CCK8 peptide for selective delivery, were developed. The peptide contg. supramol. aggregates were obtained by mixing two different amphiphilic monomers: one of them contg. a chelating agent able to complex a metal ion and the other the bioactive CCK8 peptide able to bind, with nanomolar affinity, cholecystokinin subtype receptors. In vitro and in vivo biol. tests on 111In labeled vesicles confirm that peptide contg. supramol. aggregates give the desired specific receptor targeting, thus indicating that CCK8 peptide adopts the expected conformation also when it is bound to supramol. aggregates. The demonstrated efficiency of surface exposed peptides in homing nanovectors to a specific target, the long plasma half-life and the no acute toxicity of the studied aggregates, give promising opportunities for the development of pharmaceutical agents with high specificity toward the biol. target and reduced toxic side effects on non-target organs.