Transdermal Penetration of Synthetic Peptides and Their Penetration Enhancement Caused by Some Terpene Compounds

[摘要] The work presented in this paper represents a study of the rate and extent of transdermal penetration of three synthetic hexapeptides consisting only of glycine (Gly) and phenylalanine (Phe) as the constituent amino acids and they include Phe-Gly-Gly-Gly-Gly-Gly (Pep-1), Phe-Phe-Gly-Gly-Gly-Gly (Pep-2), and Phe-Phe-Phe- Gly-Gly-Gly (Pep-3). The present study demonstrated the extent to which the peptides having a high metabolic stability were transdermally transported from the various vehicles. The results of this study appear to indicate that minor differences in the lipophilicity of the synthetic hexapeptides have a slight influence on the rate and extent of transport. In the presence of terpene permeation enhancers, together with ethanol (i.e., menthone/ EtOH, carveol/EtOH or cineole/EtOH), the peptides were more rapidly penetrated through the skin and among the terpenes tested, cineole was the most effective for all three peptides. The maximum enhancement ratio of approximately 2 was achieved by cineole in 50% ethanol solution.

[学科分类] 化学（综合）

[关键词] Transdermal;Synthetic peptide;Permeation enhancer;Terpene