Self-Assembled Palmitoyl-Glycine-Histidine as a Permeation Enhancer for Transdermal Delivery

Takayuki Imoto, Masahiro Goto

Research output: Contribution to journalArticlepeer-review

Abstract

The stratum corneum (SC) covers the outer surface of the skin and prevents the permeation of unwanted materials; however, the SC barrier also inhibits the desired permeation of active pharmaceutical ingredients (APIs). Therefore, the development of a novel method to enhance the permeation of APIs through the skin has been the focus of significant attention. Palmitoyl-glycine-histidine (Pal-GH) - comprising palmitic acid, glycine, and histidine - can be co-assembled with various additives to form a thixotropic hydrogel. Self-assembled Pal-GH enhances the permeation of ivermectin through the skin; however, the permeation mechanism is unclear and has not yet been discussed in detail. In the present study, the self-assembled structure of Pal-GH was analyzed using X-rays and infrared, and its permeation enhancement effect was verified. There was a correlation between the amount of Pal-GH in the skin and permeation enhancement, suggesting the involvement of the Pal-GH molecule. The presence of Pal-GH in the skin was confirmed by liquid chromatography-mass spectrometry and fluorescence labeling (labeling with Thioflavin T, a fluorescent dye that responds to β-sheets). The self-assembled Pal-GH permeated the SC without disrupting its organization. However, the structure of the Pal-GH caused changes to the lipid organization of the SC. The findings indicated that self-assembled Pal-GH is an effective permeation enhancer for transdermal delivery and does not induce skin irritation.

Original languageEnglish
Pages (from-to)8971-8977
Number of pages7
JournalLangmuir
Volume37
Issue number30
DOIs
Publication statusPublished - Aug 3 2021

All Science Journal Classification (ASJC) codes

  • Materials Science(all)
  • Condensed Matter Physics
  • Surfaces and Interfaces
  • Spectroscopy
  • Electrochemistry

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