Abstract
Purpose. The aim was to assess the feasibility of cutaneousmicrodialysis as a method to study percutaneous penetration of methyl nicotinatethrough human skin in vitro and in vivo.
Methods. Microdialysis was applied in vitro in excised human skin,in isolated dermis, in reconstructed human epidermis and in vivo inthe volar forearm skin of volunteers using methyl nicotinate (MN) asa model compound. After topical application of MN, aliquots of theperfusate were collected and analyzed for the presence of MNspectrophotometrically and by HPLC. In vivo, visual scoring and laser Dopplerperfusion imaging (LDPI) were used to monitor the effects on skinblood flow.
Results. In vitro, MN was detected in the dialysate after a 1 minexposure of excised skin to concentrations as low as 25 mM. Higherconcentrations up to 500 mM showed increased levels. Prolongationof the application time to 60 min resulted in increased levels of MNin the perfusate as the duration of application increased. Reconstructedepidermis and isolated dermis showed an almost 2- and 20-fold higherpenetration compared to excised skin, respectively. In vivo, LDPImeasurements showed a rapid increase in skin blood flow afterapplication of 25 to 100 mM MN for 1 min. MN was only detectable inthe microdialysate after application of 100 mM for 10 min (two ofthree subjects).
Conclusions. Cutaneous microdialysis may be a tool for comparativestudies linking responses in human skin in vivo to in vitro data usingthe same technique and endpoint.
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Boelsma, E., Anderson, C., Karlsson, A.M.J. et al. Microdialysis Technique as a Method to Study the Percutaneous Penetration of Methyl Nicotinate Through Excised Human Skin, Reconstructed Epidermis, and Human Skin In Vivo. Pharm Res 17, 141–147 (2000). https://doi.org/10.1023/A:1007505011474
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DOI: https://doi.org/10.1023/A:1007505011474