Triggered release from peptide-proteinoid microspheres.

Abstract

Proteinoid microspheres (PM) are unusual polymers formed by the thermal condensation of amino acids. Although they have been studied for over 60 years, they are only now beginning to garner interest as controlled release agents. Although they are very biocompatible, it has been problematic to design useful triggers that release small molecules from PM interiors. This has severely limited their usefulness. In the present study, short peptides have been successfully incorporated into PMs during their formation. The resulting hybrid peptide-PMs can release their interior content when hydrolyzed by a proteinase. Specifically, if a matrix metalloproteinase (MMP) cleavage site peptide is incorporated into a PM, the peptide-PM will release interior contents only in the presence of the MMP recognizing the cleavage peptide. The release rate can be determined by the concentration of the peptide in the PM synthesis mixture. This potentially makes peptide-PMs useful for delivering inhibitors or drugs into acute and chronic wounds, periodontal disease sites, and other disease states involving the fine-tuned regulation of proteinases.