Development, Characterization and Skin Interaction of Capsaicin-Loaded Microemulsion-Based Nonionic Surfactant

Biol Pharm Bull. 2016;39(4):601-10. doi: 10.1248/bpb.b15-00961.

Abstract

The aim of this study was to develop novel microemulsions (MEs) for the transdermal delivery of capsaicin. Microemulsion-based nonionic surfactants consisting of isopropyl myristate as the oil phase, various nonionic surfactants as the surfactant (S), various glycols or alcohol as the co-surfactant (CoS), and reverse osmosis water as the aqueous phase were formulated. Based on the optimal ME obtained from Design Expert, MEs containing a fixed concentration of oil, water or surfactant were prepared while varying the amounts of the other two fractions. The results indicated that the skin permeation flux of low dose capsaicin (0.15% (w/w)) was significantly higher for the selected ME than the commercial product and capsaicin in ethanol (control) by approximately two- and four-fold, respectively. We successfully demonstrated the feasibility of the transdermal delivery of capsaicin-loaded ME using a low concentration of nonionic surfactant and ethanol. Moreover, the optimization using computer program helped to simplify the development of a pharmaceutical product.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Capsaicin / administration & dosage*
  • Capsaicin / chemistry
  • Capsaicin / pharmacokinetics
  • Electric Conductivity
  • Emulsions
  • Ethanol / administration & dosage
  • Ethanol / chemistry
  • Ethanol / pharmacokinetics
  • Female
  • Glucosides / administration & dosage
  • Glucosides / chemistry
  • Glucosides / pharmacokinetics
  • In Vitro Techniques
  • Mice
  • Myristates / administration & dosage
  • Myristates / chemistry
  • Myristates / pharmacokinetics
  • Polyethylene Glycols / administration & dosage
  • Polyethylene Glycols / chemistry
  • Polyethylene Glycols / pharmacokinetics
  • Skin / metabolism*
  • Skin Absorption
  • Surface-Active Agents / administration & dosage*
  • Surface-Active Agents / chemistry
  • Surface-Active Agents / pharmacokinetics
  • Water / administration & dosage
  • Water / chemistry

Substances

  • Emulsions
  • Glucosides
  • Myristates
  • Surface-Active Agents
  • Water
  • isopropyl myristate
  • Ethanol
  • Polyethylene Glycols
  • Capsaicin
  • decyl glucoside