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Transdermal permeation modulation by cyclodextrins: a mechanistic study

A C Williams1, S R Shatri, B W Barry

  • 1School of Pharmacy, University of Bradford, West Yorkshire, UK. A.C.Williams@bradford.ac.uk

Pharmaceutical Development and Technology
|September 22, 1998
PubMed
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Beta- and 2-hydroxypropyl-beta-cyclodextrins (HP-beta-CD) do not enhance drug permeation through skin. However, these cyclodextrins (CDs) can be used in barrier creams to reduce toxic toluene absorption.

Area of Science:

  • Pharmaceutical Sciences
  • Dermatology
  • Toxicology

Background:

  • Cyclodextrins (CDs) are widely used in drug delivery.
  • Their potential as penetration enhancers or in protective formulations requires investigation.

Purpose of the Study:

  • To evaluate beta- and 2-hydroxypropyl-beta-cyclodextrins (beta-CD and HP-beta-CD) as permeation modulators for 5-fluorouracil and estradiol.
  • To assess the efficacy of CDs in a barrier cream against toluene exposure.

Main Methods:

  • Phase solubility studies, permeation experiments, and thermal analysis of stratum corneum.
  • Characterization of inclusion complexes using Karl Fischer titrimetry, infrared spectroscopy, and thermal analysis.

Main Results:

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  • HP-beta-CD formed soluble complexes with terpenes and toluene, unlike beta-CD.
  • CDs did not enhance drug flux; estradiol permeation decreased after CD pretreatment.
  • CD-terpene complexes showed reduced enhancer efficacy.
  • Both CDs, especially beta-CD, retarded toluene permeation in a barrier ointment.

    • Conclusions:

    • CDs are not penetration enhancers for 5-fluorouracil or estradiol in human skin.
    • CDs show potential in barrier formulations to limit occupational exposure to toxic substances.