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Influence of Lipophilic Counter-Ions in Combination With Phloretin and 6-ketocholestanol on the Skin Permeation of 5-aminolevulinic Acid

Influence of Lipophilic Counter-Ions in Combination With Phloretin and 6-ketocholestanol on the Skin Permeation of 5-aminolevulinic Acid

B G Auner, C Valenta, J Hadgraft

Int J Pharm. 2003 Apr 14;255(1-2):109-16.

PMID: 12672607

Abstract:

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 (logP(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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP207596290	Sodium 1-octanesulfonate monohydrate		207596-29-0	Price
AP207605401	Sodium 1-pentanesulfonate monohydrate		207605-40-1	Price

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