The physicochemical characterization and in vitro/in vivo evaluation of natural surfactants-based emulsions as vehicles for diclofenac diethylamine

Drug Dev Ind Pharm. 2007 Mar;33(3):221-34. doi: 10.1080/03639040601150179.

Abstract

Two sugar-based emulsifiers, cetearyl alcohol & cetearyl glycoside and sorbitan stearate & sucrose cocoate, known as potential promoters of lamellar liquid crystals/gel phases, were investigated in order to formulate an optimal vehicle for amphiphilic drug - diclofenac diethylamine (DDA). Physico-chemical characterization and study of vehicle's physical stability were performed. Then, the in vitro DDA liberation profile, dependent on the mode of drug incorporation to the system, and the in vivo, short-term effects of chosen samples on skin parameters were examined. Droplets size distribution and rheological behavior indicated satisfying physical stability of both types of vehicles. Unexpectedly, the manner of DDA incorporation to the system had no significant influence on DDA release. In vivo study pointed to emulsion's favorable potential for skin hydration and barrier improvement, particularly in cetearyl glycoside-based vehicle.

Publication types

  • Evaluation Study

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Chemistry, Pharmaceutical / methods*
  • Diclofenac / administration & dosage
  • Diclofenac / pharmacokinetics*
  • Diethylamines / administration & dosage
  • Diethylamines / pharmacokinetics*
  • Emulsions*
  • Fatty Alcohols / chemistry*
  • Glucosides / chemistry*
  • Humans
  • Liquid Crystals
  • Rheology
  • Skin Absorption
  • Stearates / chemistry*
  • Surface-Active Agents / chemistry*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Diethylamines
  • Emulsions
  • Fatty Alcohols
  • Glucosides
  • Stearates
  • Surface-Active Agents
  • Diclofenac
  • cetearyl alcohol
  • diethylamine