Physicochemical performances of indomethacin in cholesteryl cetyl carbonate liquid crystal as a transdermal dosage

AAPS PharmSciTech. 2012 Jun;13(2):513-21. doi: 10.1208/s12249-012-9768-5. Epub 2012 Mar 20.

Abstract

A transdermal formulation of indomethacin (IMC) was developed by incorporation into cholesteryl cetyl carbonate (CCC). The liquid crystalline phase properties of the IMC-CCC mixture were detected by polarized light microscopy and differential scanning calorimetry. A low drug loading was obtained (1-5 %) similar to that used in conventional topical IMC in a clinical setting. A controlled release of IMC was found over 12 h. A low amount of IMC in 1 % IMC-CCC permeated the stratum corneum. Further formulation development has been carried out by the addition of lauryl alcohol into 5 % IMC-CCC mixture it was found that the permeation of IMC was significantly improved to 45 % within 24 h.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Animals, Newborn
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / metabolism
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Cholesterol Esters / chemistry*
  • Delayed-Action Preparations
  • Dodecanol / chemistry
  • Drug Carriers*
  • Drug Stability
  • Hydrogen-Ion Concentration
  • Indomethacin / administration & dosage*
  • Indomethacin / chemistry
  • Indomethacin / metabolism
  • Kinetics
  • Liquid Crystals
  • Microscopy, Polarization
  • Permeability
  • Skin / metabolism
  • Skin Absorption
  • Skin Temperature
  • Solubility
  • Swine
  • Technology, Pharmaceutical / methods
  • Transition Temperature

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cholesterol Esters
  • Delayed-Action Preparations
  • Drug Carriers
  • cholesteryl cetyl carbonate
  • Dodecanol
  • Indomethacin