
pmid: 15544867
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 80-100 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.
Y-Aminolevulinic acid, Sponge phase, Methyl ester, Swine, Biological Transport, Aminolevulinic Acid, Buffers, In Vitro Techniques, Iontophoresis, Administration, Cutaneous, Monoolein, Excipients, Solutions, 615, Liposomes, Transdermal delivery, Animals, Diffusion Chambers, Culture, Spectrophotometry, Ultraviolet, Ear, External, Skin
Y-Aminolevulinic acid, Sponge phase, Methyl ester, Swine, Biological Transport, Aminolevulinic Acid, Buffers, In Vitro Techniques, Iontophoresis, Administration, Cutaneous, Monoolein, Excipients, Solutions, 615, Liposomes, Transdermal delivery, Animals, Diffusion Chambers, Culture, Spectrophotometry, Ultraviolet, Ear, External, Skin
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