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Transdermal behaviour of the N-alkylamide spilanthol

Jente Boonen UGent, Eline Halet UGent, Christian Burvenich UGent, Phillip Blondeel UGent and Bart De Spiegeleer UGent (2009)
abstract
N-alkylamides are a group of bioactive molecules found in several plants from the geni Echinacea, Xanthoxylum and Spilanthes. Extracts and formulations derived from these plants are not only orally used but are applied on the skin as well. However, there is no specific information available about the intrinsic local pharmacokinetics of N-alkylamides after topical application on human skin, questioning the role of this mode of administration. Therefore, we have investigated the transdermal behavior of spilanthol as N-alkylamide model compound. Two pharmaceutically accepted vehicles (ethanol and propylene glycol based aqueous solutions), combined with three different receptor fluids (PBS, PBS/HPBCD, EtOH/H2O), were applied on split-thickness human skin in a Franz diffusion system. However, seen the confounding penetration modifying effects of those solvents, the permeation characteristics of spilanthol in a solvent-independent (100% aqueous dose solution) way was also obtained using an extrapolation approach with different organic solvent/H2O ratios. It was shown that spilanthol did permeate the skin. Partitioning (Km) was strongly dependent on the donor-vehicle composition, while diffusion (Dm) was mainly influenced by the receptor fluid composition. The following extrapolated quantitative primary parameters were obtained (mean ± SEM): Kp,aq = 3.31 ∙ 10-3 ± 0.28 ∙ 10-3 cm/h, Dm, aq = 1.90 ∙ 10-4 ± 0.07 ∙ 10-4 cm²/h and Km, aq = 7.27 ∙ 10-1 ± 1.56 ∙ 10-1 [1]. References [1] J. Boonen, B. Baert, N. Roche, C. Burvenich and B. De Spiegeleer. Transdermal behaviour of the N-alkylamide spilanthol (affinin) from Spilanthes acmella (Compositae) extracts, 2009, publication submitted.
Please use this url to cite or link to this publication:
author
organization
year
type
conference
publication status
published
subject
pages
1 pages
conference name
Symposium
conference location
Faculty of Pharmaceutical Sciences, Ghent University
conference start
2009-05-20
language
English
UGent publication?
yes
classification
C3
id
666472
handle
http://hdl.handle.net/1854/LU-666472
date created
2009-05-26 13:29:30
date last changed
2016-12-19 15:35:17
@inproceedings{666472,
  abstract     = {N-alkylamides are a group of bioactive molecules found in several plants from the geni Echinacea, Xanthoxylum and Spilanthes. Extracts and formulations derived from these plants are not only orally used but are applied on the skin as well. However, there is no specific information available about the intrinsic local pharmacokinetics of N-alkylamides after topical application on human skin, questioning the role of this mode of administration. Therefore, we have investigated the transdermal behavior of spilanthol as N-alkylamide model compound.
Two pharmaceutically accepted vehicles (ethanol and propylene glycol based aqueous solutions), combined with three different receptor fluids (PBS, PBS/HPBCD, EtOH/H2O), were applied on split-thickness human skin in a Franz diffusion system. However, seen the confounding penetration modifying effects of those solvents, the permeation characteristics of spilanthol in a solvent-independent (100\% aqueous dose solution) way was also obtained using an extrapolation approach with different organic solvent/H2O ratios.
It was shown that spilanthol did permeate the skin. Partitioning (Km) was strongly dependent on the donor-vehicle composition, while diffusion (Dm) was mainly influenced by the receptor fluid composition. The following extrapolated quantitative primary parameters were obtained (mean {\textpm} SEM): Kp,aq = 3.31 \unmatched{2219} 10-3 {\textpm} 0.28 \unmatched{2219} 10-3 cm/h, Dm, aq = 1.90 \unmatched{2219} 10-4 {\textpm} 0.07 \unmatched{2219} 10-4 cm{\texttwosuperior}/h and Km, aq = 7.27 \unmatched{2219} 10-1 {\textpm} 1.56 \unmatched{2219} 10-1 [1].

References
[1] J. Boonen, B. Baert, N. Roche, C. Burvenich and B. De Spiegeleer. Transdermal behaviour of the N-alkylamide spilanthol (affinin) from Spilanthes acmella (Compositae) extracts,  2009, publication submitted.},
  author       = {Boonen, Jente and Halet, Eline and Burvenich, Christian and Blondeel, Phillip and De Spiegeleer, Bart},
  language     = {eng},
  location     = {Faculty of Pharmaceutical Sciences, Ghent University},
  pages        = {1},
  title        = {Transdermal behaviour of the N-alkylamide spilanthol},
  year         = {2009},
}

Chicago
Boonen, Jente, Eline Halet, Christian Burvenich, Phillip Blondeel, and Bart De Spiegeleer. 2009. “Transdermal Behaviour of the N-alkylamide Spilanthol.” In .
APA
Boonen, Jente, Halet, E., Burvenich, C., Blondeel, P., & De Spiegeleer, B. (2009). Transdermal behaviour of the N-alkylamide spilanthol. Presented at the Symposium.
Vancouver
1.
Boonen J, Halet E, Burvenich C, Blondeel P, De Spiegeleer B. Transdermal behaviour of the N-alkylamide spilanthol. 2009.
MLA
Boonen, Jente, Eline Halet, Christian Burvenich, et al. “Transdermal Behaviour of the N-alkylamide Spilanthol.” 2009. Print.