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Effect of oligoarginine conjugation on the antiwrinkle activity and transdermal delivery of GHK peptide
Author(s) -
Hur GaHee,
Han SangCheol,
Ryu AReum,
Eom Youngsic,
Kim JhinWook,
Lee MiYoung
Publication year - 2020
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.3234
Subject(s) - transdermal , cosmeceutical , in vitro , in vivo , peptide , chemistry , pharmacology , matrix metalloproteinase , human skin , biochemistry , medicine , biology , pathology , genetics , microbiology and biotechnology
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, Arg 4 was 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, Arg 4 conjugation 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.