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

Nadia Merclin ; Johanna Bender (Institutionen för material- och ytkemi, Teknisk ytkemi) ; Emma Sparr ; Richard Guy ; Hans Ehrsson ; Sven Engström (Institutionen för material- och ytkemi, Teknisk ytkemi)
Journal of Controlled Release (0168-3659). Vol. 100 (2004), 2, p. 191-198.
[Artikel, refereegranskad vetenskaplig]

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(R) (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 80-100 nmol 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.

Nyckelord: Sponge phase, Monoolein, delta-Aminolevulinic acid methyl ester, Transdermal delivery, Iontophoresis

Denna post skapades 2006-08-29. Senast ändrad 2013-05-22.
CPL Pubid: 12825


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Institutionen för material- och ytkemi, Teknisk ytkemi (2002-2004)


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