Profiling skin penetration using PEGylated emulsifiers as penetration enhancers via confocal Raman spectroscopy and fluorescence spectroscopy

Eur J Pharm Biopharm. 2021 Sep:166:1-9. doi: 10.1016/j.ejpb.2021.04.027. Epub 2021 Jun 1.

Abstract

Non-ionic emulsifiers have been continuous research focus in skin analysis. With the aim of finding their role as penetration enhancers in dermal drug delivery systems, PEGylated emulsifiers of polyethylene glycol (PEG) ethers were targeted to be investigated ex-vivo. The effectiveness of them in the enhancement of skin penetration was examined by conventional tape stripping method and confocal Raman spectroscopy (CRS). Fluorescein sodium salt (Fluo-Na) and procaine HCl were respectively used as model drugs. The drug delivery performances were compared in the aspects of penetration amount and depth. Based on the results from both analyses, all investigated emulsifiers have the ability to enhance the amount of drug penetration. PEG-20 ethers showed higher ability than PEG-2 oleyl ether (O2) in promoting drug distribution by depth, especially PEG-20 cetyl ether (C20) showed a distinct effect. According to this study, their penetration enhancing performances seem to be linked to their interruption of intercellular lipids, which can be considered as the underlying mechanism for governing the ability of PEGylated emulsifiers as penetration enhancers. Further instrumental comparison highlighted the benefits of using CRS as an alternative in skin penetration analysis.

Keywords: Confocal Raman spectroscopy; Fluorescein sodium salt; PEGylated emulsifiers; Procaine HCl; Tape stripping.

MeSH terms

  • Animals
  • Drug Delivery Systems / methods
  • Emulsifying Agents / pharmacology*
  • Lipid Metabolism / drug effects
  • Plant Oils / pharmacology*
  • Polyethylene Glycols / pharmacology*
  • Skin / drug effects
  • Skin Absorption* / drug effects
  • Skin Absorption* / physiology
  • Spectrometry, Fluorescence / methods*
  • Spectrum Analysis, Raman / methods*
  • Surface-Active Agents / pharmacology
  • Swine

Substances

  • Emulsifying Agents
  • Plant Oils
  • Surface-Active Agents
  • Polyethylene Glycols
  • polyethylene glycol oleyl ether