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Skin penetration enhancing effect of the plant N-alkylamide spilanthol

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Organization
Abstract
Objective : N-alkylamides are secondary metabolites of plants often used in topical preparations (Alkamid database). The question posed was if, and to what extent, these N-alkylamides influence the permeation behavior of accompanying or skin-contacting compounds. Methodology : Spilanthol was used as model N-alkylamide, and its effect on human skin permeation of 3 model compounds (caffeine, testosterone, ibuprofen in water/ethanol 50/50%) was investigated with an ex-vivo in-vitro static Franz diffusion cell (FDC) method, measuring the flux over 24 hours. Moreover, a concentration-effect relationship was investigated over 0.05% to 2% spilanthol concentration. The influence of spilanthol on the transdermal behavior of some mycotoxines (aflatoxin B1, ochratoxin A, fumonisin B1, citrinin, zearalenone and T-2 toxin) was also investigated in a similar FDC set-up. Results : The enhancement ratio (ER) of spilanthol on caffeine and testosterone permeability coefficient (Kp) was 4.9, resp. 2.9, while no significant effect on ibuprofen (ER of 1.1) was observed. A concentration dependent ER-response was observed, with ER values ranging between 1.9 (0.05% spilanthol) to 4.9 (up to 2% spilanthol). The toxicological-clinical consequences of our findings is exemplified by the enhancement of skin permeation of the six model mycotoxines , hazardous fungal compounds ubiquitous present in our environment, including in plants containing these N-alkylamides. Conclusions : Some plant constituents, like the N-alkylamide spilanthol, do significantly increase the permeation properties of the skin towards other compounds. This may clinically influence the functionality and toxicity of these compounds.
Keywords
N-alkylamide, skin penetration enhancing effect, spilanthol, mycotoxines

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Chicago
De Spiegeleer, Bart, Jente Boonen, Lieselotte Veryser, Lien Taevernier, Svetlana Malysheva, José Diana Di Mavungu, and Sarah De Saeger. 2012. “Skin Penetration Enhancing Effect of the Plant N-alkylamide Spilanthol.” In International Journal of Cosmetic Science, 34:383–383.
APA
De Spiegeleer, B., Boonen, J., Veryser, L., Taevernier, L., Malysheva, S., Diana Di Mavungu, J., & De Saeger, S. (2012). Skin penetration enhancing effect of the plant N-alkylamide spilanthol. INTERNATIONAL JOURNAL OF COSMETIC SCIENCE (Vol. 34, pp. 383–383). Presented at the Stratum Corneum VII.
Vancouver
1.
De Spiegeleer B, Boonen J, Veryser L, Taevernier L, Malysheva S, Diana Di Mavungu J, et al. Skin penetration enhancing effect of the plant N-alkylamide spilanthol. INTERNATIONAL JOURNAL OF COSMETIC SCIENCE. 2012. p. 383–383.
MLA
De Spiegeleer, Bart, Jente Boonen, Lieselotte Veryser, et al. “Skin Penetration Enhancing Effect of the Plant N-alkylamide Spilanthol.” International Journal of Cosmetic Science. Vol. 34. 2012. 383–383. Print.
@inproceedings{2970123,
  abstract     = {Objective : N-alkylamides are secondary metabolites of plants often used in topical preparations (Alkamid database). The question posed was if,  and to what extent, these N-alkylamides influence the permeation behavior of accompanying or skin-contacting compounds.
Methodology : Spilanthol was used as model N-alkylamide, and its effect on human skin permeation of 3 model compounds (caffeine, testosterone, ibuprofen in water/ethanol 50/50\%) was investigated with an ex-vivo in-vitro static Franz diffusion cell (FDC) method, measuring the flux over 24 hours. Moreover, a concentration-effect relationship was investigated over 0.05\% to 2\% spilanthol concentration.
The influence of spilanthol on the transdermal behavior of some mycotoxines (aflatoxin B1, ochratoxin A, fumonisin B1, citrinin, zearalenone and T-2 toxin) was also investigated in a similar FDC set-up.
Results : The enhancement ratio (ER) of spilanthol on caffeine and testosterone permeability coefficient (Kp) was 4.9, resp. 2.9, while no significant effect on ibuprofen (ER of 1.1) was observed. A concentration dependent ER-response was observed, with ER values ranging between 1.9 (0.05\% spilanthol) to 4.9 (up to 2\% spilanthol). The toxicological-clinical consequences of our findings is exemplified by the enhancement of skin permeation of the six model mycotoxines , hazardous fungal compounds ubiquitous present in our environment, including in plants containing these N-alkylamides.
Conclusions : Some plant constituents, like the N-alkylamide spilanthol, do significantly increase the permeation properties of the skin towards other compounds. This may clinically influence the functionality and toxicity of these compounds.},
  author       = {De Spiegeleer, Bart and Boonen, Jente and Veryser, Lieselotte and Taevernier, Lien and Malysheva, Svetlana and Diana Di Mavungu, Jos{\'e} and De Saeger, Sarah},
  booktitle    = {INTERNATIONAL JOURNAL OF COSMETIC SCIENCE},
  issn         = {0142-5463},
  language     = {eng},
  location     = {Cardiff, Wales, UK},
  number       = {4},
  pages        = {383--383},
  title        = {Skin penetration enhancing effect of the plant N-alkylamide spilanthol},
  volume       = {34},
  year         = {2012},
}

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