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((R))CC, Labrafil((R)), Labrasol((R)) and Transcutol((R)) 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 21K MAL whereas for 10% and 20% (wt./wt.) MAL concentrations only DMSO, HPE-101 and Labrafac((R))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((R))CC to reduce skin irritation induced by HPE-101 without impairing the porphyrin formation. (c) 2005 Elsevier B.V. All rights reserved.