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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

Merclin, N; Bender, J; Sparr, Emma LU ; Guy, R H; Ehrsson, H and Engström, S (2004) In Journal of Controlled Release 100(2). p.191-198
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(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... (More)
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. (C) 2004 Elsevier B.V. All rights reserved. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Controlled Release
volume
100
issue
2
pages
191 - 198
publisher
Elsevier
external identifiers
  • pmid:15544867
  • wos:000225847700004
  • scopus:8544222780
ISSN
1873-4995
DOI
10.1016/j.jconrel.2004.08.025
language
English
LU publication?
yes
id
537f648a-ac8e-4b16-af0e-64ea55f45699 (old id 154027)
date added to LUP
2007-07-11 16:32:34
date last changed
2017-01-01 04:46:52
@article{537f648a-ac8e-4b16-af0e-64ea55f45699,
  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(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. (C) 2004 Elsevier B.V. All rights reserved.},
  author       = {Merclin, N and Bender, J and Sparr, Emma and Guy, R H and Ehrsson, H and Engström, S},
  issn         = {1873-4995},
  language     = {eng},
  number       = {2},
  pages        = {191--198},
  publisher    = {Elsevier},
  series       = {Journal of Controlled Release},
  title        = {Transdermal delivery from a lipid sponge phase-iontophoretic and passive transport in vitro of 5-aminolevulinic acid and its methyl ester},
  url          = {http://dx.doi.org/10.1016/j.jconrel.2004.08.025},
  volume       = {100},
  year         = {2004},
}