Transdermal Delivery and Biological Activity of Arginine Oligomer Conjugation of Palmitoyl Tripeptide-1

GHK is a promising cosmeceutical peptide that stimulates the synthesis of ECM and modulates activity Matrix Metallo Proteinases (MMPs). However, due to hydrophilic properties GHK, skin permeability challenge. To overcome this limitation, we considered two modifications, namely palmitoyl attachment arginine oligomer conjugation. First, evaluated optimal modification for penetration using Franz diffusion cell assay with 3D human reconstructed skin. We found was slightly increased by attaching at N-terminus while it significantly conjugating oligomers C-terminus GHK. In comparison between R4, R6, R8, R4 showed highest penetrating potential, Pal-GHK-R4 about 7-fold higher than Based on results, peptide, Pal-GHK-R4, synthesized SPPS, after which its biological activities were verified. Evaluating MMP-2 gelatin zymography collagen production Sircol had approximately100-fold lower active concentrations other words, established novel as increases both