The effect of skin permeation enhancers on the formation of porphyrins in mouse skin during topical application of the methyl ester of 5-aminolevulinic acid.
The influence of skin permeation enhancers, such as dimethyl sulphoxide (DMSO) and 1-[2-(decylthio)ethyl]azacyclopentan-2-one (HPE-101), Labrafac CC, Labrafil, Labrasol and Transcutol in a concentration of 10% (wt./wt.) on the formation of porphyrins in normal mouse skin from topical application of creams with methyl 5-aminolevulinate (MAL) was studied. The concentration of porphyrins in the mouse skin was determined by direct fluorescence measurements. The results show that studied permeation enhancers increase the formation of porphyrins, and therefore also the skin penetration 2% MAL whereas for 10% and 20% (wt./wt.) MAL concentrations only DMSO, HPE-101 and Labrafac CC increased the porphyrin formation. At all studied MAL concentrations DMSO gave the largest enhancing effect, similarly to that of HPE-101. This suggests that in 2-20% MAL creams HPE-101 may be substituted by Labrafac CC to reduce skin irritation induced by HPE-101 without impairing the porphyrin formation.
Bugaj
Andrzej
A
Department of Clinical Pharmacy and Biopharmacy, Karol Marcinkowski University of Medical Sciences, ul. Marii Magdaleny 14, 61861 Poznań, Poland. andrzejbugaj@yahoo.fr
Juzeniene
Asta
A
Juzenas
Petras
P
Iani
Vladimir
V
Ma
Li Wei
LW
Moan
Johan
J
D000287:Administration, Topical; D000622:Aminolevulinic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives*; D000818:Animals; D004121:Dimethyl Sulfoxide / Q000008:administration & dosage; D005260:Female; D005453:Fluorescence; D007700:Kinetics; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D010539:Permeability / Q000187:drug effects; D010778:Photochemotherapy; D011166:Porphyrins / Q000096:biosynthesis*; D011758:Pyrroles / Q000008:administration & dosage; D012867:Skin / Q000187:drug effects* / Q000378:metabolism*
D011166:Porphyrins; D011758:Pyrroles; C114767:delta-aminolevulinic acid methyl ester; D000622:Aminolevulinic Acid; C075725:1-(2-(decylthio)ethyl)azacyclopentane-2-one; D004121:Dimethyl Sulfoxide