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Transdermal penetration enhancing effect of the N-alkylamide spilanthol

Jente Boonen (UGent) , Lieselotte Veryser (UGent) , Lien Taevernier (UGent) , Nathalie Roche (UGent) and Bart De Spiegeleer (UGent)
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Abstract
The dermal penetration of compounds may be influenced by other compounds when mixtures are presented to the skin. Plant extracts, often used in cosmeceuticals, are complex mixtures of wanted bio-actives as well as undesirable impurities like nanoparticles and mycotoxines. A major question is if plant bio-actives (like spilanthol) can significantly alter the dermal penetration of other compounds which can be actives (like testosterone) or impurities (like mycotoxins). If so, the qualification assessment of the product quality needs to include this influence within the Quality-by-Design strategy. Therefore, the concentration-dependent penetration promoting effect of spilanthol was investigated on the three CART transdermal model compounds i.e. caffeine, ibuprofen and testosterone [1]. It was shown that spilanthol has a compound and concentration dependent penetration enhancing effect. No significant penetration enhancing effect for ibuprofen has been observed. However, with increasing spilanthol concentration (from 0 up to 1%, m/V), the permeability of caffeine increases, resulting in an enhancing ratio (ER) of 4.60 ± 0.49 (mean ± SEM, n=4). For testosterone, a maximal penetration enhancing concentration of 0.5% spilanthol was found (ER = 4.13 ± 0.44 (mean ± SEM, n=3)). Our findings with these model compounds are also confirmed with mycotoxins [2]. In conclusion, the existence of a significant mutual influence of compounds towards skin penetration should always be considered as part of the functional quality evaluation or in topical product development. References [1] B. Baert, E. Deconinck, M. Van Gele, M. Slodicka, P. Stoppie, S. Bode, G. Slegers, Y. Vander Heyden, J. Lambert, J. Beetens, B. De Spiegeleer. Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds, 2007, Bioorganic & medicinal chemistry, 15(22): 6943-6955. [2] B. De Spiegeleer, J. Boonen, L. Veryser, L. Taevernier, S.V. Malysheva, J. Diana Di Mavungu, S. De Saeger, N. Roche, P. Blondeel. Skin penetration enhancing properties of the plant N-alkylamide spilanthol, 2012, manuscript in preparation.

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Chicago
Boonen, Jente, Lieselotte Veryser, Lien Taevernier, Nathalie Roche, and Bart De Spiegeleer. 2012. “Transdermal Penetration Enhancing Effect of the N-alkylamide Spilanthol.” In Scientific Afternoon, Posters. Ghent University. Faculty of Pharmaceutical Sciences.
APA
Boonen, Jente, Veryser, L., Taevernier, L., Roche, N., & De Spiegeleer, B. (2012). Transdermal penetration enhancing effect of the N-alkylamide spilanthol. Scientific Afternoon, Posters. Presented at the 4th Scientific afternoon, Ghent University. Faculty of Pharmaceutical Sciences.
Vancouver
1.
Boonen J, Veryser L, Taevernier L, Roche N, De Spiegeleer B. Transdermal penetration enhancing effect of the N-alkylamide spilanthol. Scientific Afternoon, Posters. Ghent University. Faculty of Pharmaceutical Sciences; 2012.
MLA
Boonen, Jente, Lieselotte Veryser, Lien Taevernier, et al. “Transdermal Penetration Enhancing Effect of the N-alkylamide Spilanthol.” Scientific Afternoon, Posters. Ghent University. Faculty of Pharmaceutical Sciences, 2012. Print.
@inproceedings{2133761,
  abstract     = {The dermal penetration of compounds may be influenced by other compounds when mixtures are presented to the skin. Plant extracts, often used in cosmeceuticals, are complex mixtures of wanted bio-actives as well as undesirable impurities like nanoparticles and mycotoxines. A major question is if plant bio-actives (like spilanthol) can significantly alter the dermal penetration of other compounds which can be actives (like testosterone) or impurities (like mycotoxins). If so, the qualification assessment of the product quality needs to include this influence within the Quality-by-Design strategy.
Therefore, the concentration-dependent penetration promoting effect of spilanthol was investigated on the three CART transdermal model compounds i.e. caffeine, ibuprofen and testosterone [1].
It was shown that spilanthol has a compound and concentration dependent penetration enhancing effect. No significant penetration enhancing effect for ibuprofen has been observed. However, with increasing spilanthol concentration (from 0 up to 1\%, m/V), the permeability of caffeine increases, resulting in an enhancing ratio (ER) of 4.60 {\textpm} 0.49 (mean {\textpm} SEM, n=4). For testosterone, a maximal penetration enhancing concentration of 0.5\% spilanthol was found (ER = 4.13 {\textpm} 0.44 (mean {\textpm} SEM, n=3)). Our findings with these model compounds are also confirmed with mycotoxins [2].
In conclusion, the existence of a significant mutual influence of compounds towards skin penetration should always be considered as part of the functional quality evaluation or in topical product development.
References
[1] B. Baert, E. Deconinck, M. Van Gele, M. Slodicka, P. Stoppie, S. Bode, G. Slegers, Y. Vander\unmatched{0009}Heyden, J. Lambert, J. Beetens, B. De Spiegeleer. Transdermal penetration behaviour of drugs:\unmatched{0009}CART-clustering, QSPR and selection of model compounds, 2007, Bioorganic \& medicinal\unmatched{0009}chemistry, 15(22): 6943-6955.
[2] B. De Spiegeleer, J. Boonen, L. Veryser, L. Taevernier, S.V. Malysheva, J. Diana Di Mavungu, S.\unmatched{0009}De Saeger, N. Roche, P. Blondeel. Skin penetration enhancing properties of the plant N-alkylamide spilanthol, 2012, manuscript in preparation.},
  author       = {Boonen, Jente and Veryser, Lieselotte and Taevernier, Lien and Roche, Nathalie and De Spiegeleer, Bart},
  booktitle    = {Scientific Afternoon, Posters},
  language     = {eng},
  location     = {Ghent, Belgium},
  publisher    = {Ghent University. Faculty of Pharmaceutical Sciences},
  title        = {Transdermal penetration enhancing effect of the N-alkylamide spilanthol},
  year         = {2012},
}