Influence of lipophilic counter-ions in combination with phloretin and 6-ketocholestanol on the skin permeation of 5-aminolevulinic acid

In this study, the effect of lipophilic counter-ions on the permeation of 5-aminolevulinic acid (ALA) in combination with skin impregnation by phloretin and 6-ketocholestanol was evaluated. Standard in vitro permeation experiments with porcine skin were performed analysing the ALA content by HPLC an...

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Bibliographic Details
Published in:International journal of pharmaceutics 2003-04, Vol.255 (1), p.109-116
Main Authors: Auner, B.G., Valenta, C., Hadgraft, J.
Format: Article
Language:English
Subjects:
5-Aminolevulinic acid
6-Ketocholestanol
Adjuvants, Pharmaceutic - pharmacology
Aminolevulinic Acid - chemistry
Aminolevulinic Acid - pharmacokinetics
Animals
Anions
Biological and medical sciences
Cations, Monovalent
Cetylpyridinium chloride
Chemistry, Pharmaceutical
Chromatography, High Pressure Liquid
Diffusion
Fluorometry
General pharmacology
Hydrogen-Ion Concentration
In Vitro Techniques
Ketocholesterols - pharmacology
Liposomes
Medical sciences
Permeability
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Phloretin
Phloretin - pharmacology
Phosphatidylcholines
Photosensitizing Agents - chemistry
Photosensitizing Agents - pharmacokinetics
Porcine skin
Skin - metabolism
Skin Absorption - drug effects
Skin, nail, hair, dermoskeleton
Swine
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Summary:In this study, the effect of lipophilic counter-ions on the permeation of 5-aminolevulinic acid (ALA) in combination with skin impregnation by phloretin and 6-ketocholestanol was evaluated. Standard in vitro permeation experiments with porcine skin were performed analysing the ALA content by HPLC and fluorescent detection after ALA derivatisation. The shake flask method in combination with a trinitrobenzensulfonic acid test for ALA analysis was performed to calculate the apparent partition coefficient (log P Oct). The permeation of ALA was enhanced by cetylpyridinium chloride and benzalkonium chloride at pH 7.0 and by sodium-1-octanesulfonic acid, sodium-1-heptanesulfonic acid and sodium-1-pentanesulfonic acid monohydrate at pH 4.0. Corresponding effects of these additives were observed on the partitioning of ALA. Pre-impregnation of porcine skin with phloretin and 6-ketocholestanol increased the ALA diffusion about 1.7-fold at pH 7.0. Moreover, this transport enhancement by 6-ketocholestanol was 3.5-fold higher when a combination of ALA and cetylpyridinium chloride was used as donor.
ISSN:0378-5173
1873-3476
DOI:10.1016/S0378-5173(03)00053-X