Design and in vitro evaluation of capsaicin transdermal controlled release cubic phase gels

AAPS PharmSciTech. 2010 Sep;11(3):1405-10. doi: 10.1208/s12249-010-9481-1. Epub 2010 Sep 14.

Abstract

The purpose of this study was to design and investigate the transdermal controlled release cubic phase gels containing capsaicin using glycerol monooleate (MO), propylene glycol (1,2-propanediol, PG), and water. Three types of cubic phase gels were designed based on the ternary phase diagram of the MO-PG-water system, and their internal structures were confirmed by polarizing light microscopy (PLM) and small-angle X-ray scattering (SAXS). Release results showed the cubic phase gels could provide a sustained system for capsaicin, while the initial water content in the gels was the major factor affecting the release rate. Release kinetics was determined to fit Higuchi's square-root equation indicating that the release was under diffusion control. The calculated diffusion exponent showed the release from cubic phase gels was anomalous transport. The unique structure of the cubic phases, capsaicin distributed in the lipid bilayers, and cubic phase gel swelling contributed to the release mechanism. The cubic phase gel may be an interesting application for transdermal delivery system of capsaicin in alleviating the post-incision pain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Capsaicin / administration & dosage*
  • Capsaicin / chemistry*
  • Delayed-Action Preparations / chemical synthesis*
  • Diffusion
  • Drug Design
  • Drug Evaluation, Preclinical
  • Gels / chemistry*
  • Phase Transition
  • Transdermal Patch*

Substances

  • Delayed-Action Preparations
  • Gels
  • Capsaicin