Microemulsion formulation design and evaluation for hydrophobic compound: Catechin topical application

Colloids Surf B Biointerfaces. 2018 Jan 1:161:121-128. doi: 10.1016/j.colsurfb.2017.10.015. Epub 2017 Oct 10.

Abstract

The aim of the present study was to design a microemulsion for catechin topical application. A mixture experimental design with five independent variables (X1: oil, X2: surfactant, X3: catechin, X4: cosurfactant and X5: water) was developed, and the response surface methodology was used to study the effect of formulation components on physiochemical characteristics and penetration capacity of a catechin-loaded microemulsion, and to obtain an optimal microemulsion formulation. The results showed that the drug-loaded microemulsion formation and characteristics were related to many parameters of the components. The transdermal amounts in receiver cells and skin deposition amount remarkably increased about 4.1-111.6-fold and 0.6-7.6-fold respectively. The lag time was significantly shortened from 10h to 1.0-6.7h. The optimal formulation with 20% surfactant, 30% cosurfactant and 2.6% Catechin was subjected to stability and irritation tests. The results showed that the physicochemical characteristics and catechin level of the drug-loaded microemulsion did not show significant degradation after 3 months of storage at 25°C.The catechin-loaded microemulsion did not cause significant irritation compared to the water-treated group.

Keywords: Catechin; Microemulsion; Mixture design; Skin irritation; Stability.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Catechin / administration & dosage*
  • Catechin / chemistry
  • Catechin / pharmacokinetics
  • Chemical Phenomena
  • Drug Design
  • Drug Evaluation, Preclinical
  • Drug Stability
  • Emulsions / chemistry*
  • Hydrophobic and Hydrophilic Interactions
  • Rats, Sprague-Dawley
  • Skin / cytology
  • Skin / metabolism*
  • Skin Absorption*
  • Surface-Active Agents / chemistry
  • Water / chemistry

Substances

  • Emulsions
  • Surface-Active Agents
  • Water
  • Catechin