Scientific article
English

Transdermal delivery from a lipid sponge phase—iontophoretic and passive transport in vitro of 5-aminolevulinic acid and its methyl ester

Published inJournal of controlled release, vol. 100, no. 2, p. 191-198
Publication date2004-11-24
First online date2004-10-08
Abstract

The hydrochloride salts of 5-aminolevulinic acid (ALA) and its methyl ester (m-ALA), respectively, were dissolved in a lipid sponge phase comprising monoolein, propylene glycol and aqueous buffer at concentrations of approximately 0.25% and 16% w/w m-ALA. The iontophoretic and passive delivery of ALA and m-ALA from this formulation through porcine skin in vitro were measured and compared to formulations used in clinical practice, 20% w/w ALA in Unguentum M and Metvix (a cream containing 16% w/w m-ALA). A sponge phase with 16% w/w m-ALA showed a higher passive flux (approximately 140 nmol cm-2 h-1 at 5 h) but a lower iontophoretic flux (approximately 800 nmol cm-2 h-1 at 5 h) compared to the clinically used products but the differences are hardly significant due to large standard deviations. ALA and m-ALA in sponge phase formulation showed iontophoretic fluxes in the range 80-100nmol cm-2 h-1 at 3 h, i.e. values comparable to the passive fluxes from the more concentrated vehicles. The results demonstrate that the lipid sponge phase, a thermodynamically stable liquid with amphiphilic character, may have potential as a transdermal drug delivery vehicle.

Keywords
  • Sponge phase
  • Monoolein
  • Y-Aminolevulinic acid
  • Methyl ester
  • Transdermal delivery
  • Iontophoresis
Citation (ISO format)
MERCLIN, N. et al. Transdermal delivery from a lipid sponge phase—iontophoretic and passive transport in vitro of 5-aminolevulinic acid and its methyl ester. In: Journal of controlled release, 2004, vol. 100, n° 2, p. 191–198. doi: 10.1016/j.jconrel.2004.08.025
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Journal ISSN0168-3659
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