Effect of oligoarginine conjugation on the antiwrinkle activity and transdermal delivery of GHK peptide.

Journal of peptide science : an official publication of the European Peptide Society2020PMID: 31788907

Animal StudyIn VitroGHK-Cu

Plain Language Summary

Investigates conjugation of oligoarginine (Arg4) to GHK to improve transdermal penetration for anti-wrinkle applications. The GHK-Arg4 heptapeptide showed significantly deeper skin penetration than GHK alone while maintaining anti-wrinkle activity in fibroblast assays. Demonstrates that peptide engineering can overcome GHK's skin permeation limitations.

Abstract

GHK (Gly-His-Lys), a natural peptide found in human skin and plasma, has been widely used in the cosmeceutical and pharmaceutical fields. The hydrophilic GHK and GHK-Cu are limited in their abilities to penetrate deeply into skin; because of this, various strategies for their skin delivery have been developed. In this investigation, Argwas conjugated with GHK to get heptapeptide, GHK-R4, and then in vitro antiwrinkle activity and transdermal delivery were compared between GHK and GHK-R4. Notably, Argconjugation accelerated the cellular penetration of GHK both in vitro and in vivo. Furthermore, higher in vitro antiwrinkle activity and collagen biosynthesis was obtained with GHK-R4 at much lower doses than with control R4-free GHK. The enhanced activity and delivery of GHK-R4 might be due to the cell penetrating ability and matrix metalloproteinase (MMP) inhibitory activity of R4 itself.

Authors

Hur, Ga-Hee; Han, Sang-Cheol; Ryu, A-Reum; Eom, Youngsic; Kim, Jhin-Wook; Lee, Mi-Young