Effects of Vehicles and Enhancers on the Skin Permeation of Phytoestrogenic Diarylheptanoids from Curcuma comosa

AAPS PharmSciTech. 2017 Apr;18(3):895-903. doi: 10.1208/s12249-016-0582-3. Epub 2016 Jul 5.

Abstract

Curcuma comosa (C. comosa) is widely used in traditional medicine as a dietary supplement for health promotion in postmenopausal women in Thailand. It contains several diarylheptanoids, which are considered to be a novel class of phytoestrogens. However, the diarylheptanoids isolated from the plant rhizome are shown to have low oral bioavailability and faster elimination characteristics. The aim of this study was to investigate the permeation behavior of the active compounds of diarylheptanoids. The effects of binary vehicle systems and permeation enhancers on diarylheptanoids permeation and accumulation within the skin were studied using side-by-side diffusion cells through the porcine ear skin. Among the tested binary vehicle systems, the ethanol/water vehicle appeared to be the most effective system for diarylheptanoids permeation with the highest flux and shortest lag time. The presence of transcutol in the vehicle system significantly increased diarylheptanoid's permeation and accumulation within the skin in a concentration-dependent manner. Although the presence of terpenes in formulation decreased the flux of diarylheptanoids, it raised the amount of diarylheptanoids retained within the skin substantially. Based on the feasibility of diarylheptanoid permeation, C. comosa extract should be further developed into an effective transdermal product for health benefits and hormone replacement therapy.

Keywords: Curcuma comosa; diarylheptanoids; permeation; skin accumulation; transepidermal water loss.

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods
  • Curcuma / chemistry*
  • Diarylheptanoids / chemistry*
  • Diarylheptanoids / metabolism*
  • Diffusion
  • Permeability
  • Pharmaceutical Vehicles / chemistry*
  • Phytoestrogens / chemistry*
  • Phytoestrogens / metabolism*
  • Plant Extracts / chemistry
  • Rhizome / chemistry
  • Skin / metabolism*
  • Skin Absorption
  • Swine
  • Terpenes / chemistry

Substances

  • Diarylheptanoids
  • Pharmaceutical Vehicles
  • Phytoestrogens
  • Plant Extracts
  • Terpenes