Topical delivery of acetyl hexapeptide-8 from different emulsions: influence of emulsion composition and internal structure

Eur J Pharm Sci. 2015 Feb 20;68:27-35. doi: 10.1016/j.ejps.2014.12.006. Epub 2014 Dec 9.

Abstract

Acetyl hexapeptide-8 (AH-8) is a well-known component of anti-aging products and was recently explored as a promising topical treatment of blepharospasm. Although AH-8 appears in a variety of cosmetic products, its skin penetration is sparsely studied and controversially discussed. Therefore, the aim of the present study was to investigate the influence of the vehicle type on the AH-8 delivery to the skin. Besides skin permeation experiments with Franz type diffusion cells, the spatial distribution of AH-8 in the stratum corneum after a real in-use application was investigated by in vitro tape stripping on porcine ear skin. By applying LC-MS/MS for quantification of AH-8, we demonstrated that a multiple water-in-oil-in-water (W/O/W) emulsion can significantly increase penetration of AH-8 into porcine skin compared to simple O/W and W/O emulsions. The internal structure of the developed multiple emulsion was confirmed by electron microscopic investigations and NMR self diffusion studies. In general, a clear superiority of water-rich W/O/W and O/W emulsions over an oil-rich W/O emulsion in terms of dermal delivery of AH-8 was found. This enhanced delivery of AH-8 could be explained by an increased absorption of the water-rich emulsions into the skin, confirmed by combined ATR-FTIR and tape stripping experiments.

Keywords: ATR-FTIR; Acetyl hexapeptide-8; Freeze–fracture; LC–MS/MS; Multiple emulsions; NMR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Emulsions
  • Glycosides / chemistry
  • In Vitro Techniques
  • Myristates / chemistry
  • Oligopeptides / administration & dosage*
  • Oligopeptides / chemistry*
  • Polyesters / chemistry*
  • Polyethylene Glycols / chemistry*
  • Skin / metabolism
  • Skin Absorption / drug effects*
  • Sucrose / analogs & derivatives*
  • Sucrose / chemistry
  • Surface-Active Agents / chemistry*
  • Swine
  • Triglycerides / chemistry
  • Water / chemistry

Substances

  • Emulsions
  • Glycosides
  • Myristates
  • Oligopeptides
  • PEG-30-dipolyhydroxystearate
  • Polyesters
  • Surface-Active Agents
  • Triglycerides
  • xylosides
  • Water
  • isopropyl myristate
  • sucrose monostearate
  • miglyol 812
  • Polyethylene Glycols
  • Sucrose
  • acetyl-glutamyl-glutamyl-methionyl-glutaminyl-arginyl-argininamide