Scientific article
English

Identification of penetration enhancers for testosterone transdermal delivery from spray formulations

Published inJournal of controlled release, vol. 113, no. 1, p. 57-62
Publication date2006-06-12
First online date2006-05-20
Abstract

The goal of this study was to identify a suitable penetration enhancer-containing formulation for the transdermal delivery of testosterone from a spray. The first step involved in vitro measurement of drug flux from a 1:1 ethanol/water saturated solution across hairless rat skin, which had been pre-treated with a series of penetration enhancers. Isopropyl myristate (IPM) was found to be the most efficient excipient, increasing testosterone transport by more than a factor of 5. The enhancing ability of IPM was also apparent when the drug was formulated in 3:1 ethanol/propylene glycol, a more compatible vehicle for use in a spray. IPM was then incorporated into this formulation directly (as opposed to being used to pre-treat the skin) over a range of concentrations from 10-25% v/v, propellant). At the highest level of enhancer, the flux was improved 2.5-fold from both the spray and the aerosol, relative to a control. However, these formulations were far from optimally conceived, in that the amount of drug which eventually contacted the skin represented only ~10% of the pulverized quantity from the spray, and ~40% of that from the aerosol. Repeated application, especially from the aerosol, improved matters somewhat, but further work is clearly required before the concept can be developed for partical application.

Citation (ISO format)
LEICHTNAM, Marie-Laure et al. Identification of penetration enhancers for testosterone transdermal delivery from spray formulations. In: Journal of controlled release, 2006, vol. 113, n° 1, p. 57–62. doi: 10.1016/j.jconrel.2006.03.008
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Journal ISSN0168-3659
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