Human skin penetration of a copper tripeptide in vitro as a function of skin layer

Inflamm Res. 2011 Jan;60(1):79-86. doi: 10.1007/s00011-010-0238-9. Epub 2010 Aug 20.

Abstract

Objective and design: Skin retention and penetration by copper applied as glycyl-L-histidyl-L-lysine cuprate diacetate was evaluated in vitro in order to assess its potential for its transdermal delivery as an anti-inflammatory agent.

Materials and methods: Flow-through diffusion cells with 1 cm(2) exposure area were used under infinite dose conditions. 0.68% aq. copper tripeptide as permeant was applied on isolated stratum corneum, heat-separated epidermis and dermatomed skin and receptor fluid collected over 48 h in 4 h intervals using inductively coupled plasma mass spectrometry to analyze for copper in tissues and receptor fluid.

Results: The permeability coefficient of the compound through dermatomed skin was 2.43 ± 0.51 × 10(-4) cm/h; 136.2 ± 17.5 μg/cm(2) copper permeated 1 cm(2) of that tissue over 48 h, while 97 ± 6.6 μg/cm(2) were retained as depot.

Conclusions: Copper as tripeptide was delivered in potentially therapeutically effective amounts for inflammatory disease.

MeSH terms

  • Acetates / chemistry
  • Acetates / pharmacology
  • Administration, Cutaneous*
  • Adult
  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Copper / chemistry
  • Copper / pharmacology*
  • Copper / therapeutic use
  • Female
  • Humans
  • Inflammation / drug therapy
  • Male
  • Middle Aged
  • Molecular Structure
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology*
  • Oligopeptides / therapeutic use
  • Permeability
  • Skin / anatomy & histology*
  • Skin / drug effects*
  • Young Adult

Substances

  • Acetates
  • Anti-Inflammatory Agents
  • Oligopeptides
  • Copper