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Amide fused-core chromatography of spilanthol as applied on a patch development

Jente Boonen (UGent) and Bart De Spiegeleer (UGent)
Author
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Abstract
For high-throughput purposes, newly developed Fused-Core HPLC stationary phases (HALO® columns) have attracted the interest of the chromatographic community. Due to their small particle size (2.7 μm) and unique particle technology with 0.5 μm porous shell fused to a solid core particle (1.7 µm diameter), these columns create fast and high performance separations. For our skin research, in vitro Franz diffusion cell (FDC) experiments are performed, resulting in large sample numbers of low concentrated bio-active in physiologic receptor media (e.g. PBS). Spilanthol, present in Spilanthes acmella as most prominent N-alkylamide and having promising transdermal activity [1, 2], could be analyzed in reversed-phase mode on the HALO® amide stationary phase with different mobile phases. Several aspects are becoming more important with these fast HPLC columns compared to the conventional columns: injection volume, sample/mobile phase solvent strength, as well as detector/data intake. We demonstrate here that all these parameters are influencing the chromatographic behaviour, and should be well defined in the method description and validation. Using Franz diffusion cells, the transdermal behaviour of spilanthol in HPMC-based patches with different percentages plasticizer (triethylcitrate (TEC)) and penetration enhancer (oleic acid (OA)) was investigated with the optimized Fused-Core method. 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, Journal of Ethnopharmacology 127(1) (2010) 77-84. [2] J. Boonen, B. Baert, C. Burvenich, P. Blondeel, S. De Saeger, B. De Spiegeleer, LC–MS profiling of N-alkylamides in Spilanthes acmella extract and the transmucosal behaviour of its main bio-active spilanthol, Journal of Pharmaceutical and Biomedical Analysis (2010), doi:10.1016/j.jpba.2010.02.010.

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Chicago
Boonen, Jente, and Bart De Spiegeleer. 2010. “Amide Fused-core Chromatography of Spilanthol as Applied on a Patch Development.” In Drug Analysis 2010, Abstracts.
APA
Boonen, Jente, & De Spiegeleer, B. (2010). Amide fused-core chromatography of spilanthol as applied on a patch development. Drug Analysis 2010, Abstracts. Presented at the Drug Analysis 2010.
Vancouver
1.
Boonen J, De Spiegeleer B. Amide fused-core chromatography of spilanthol as applied on a patch development. Drug Analysis 2010, Abstracts. 2010.
MLA
Boonen, Jente, and Bart De Spiegeleer. “Amide Fused-core Chromatography of Spilanthol as Applied on a Patch Development.” Drug Analysis 2010, Abstracts. 2010. Print.
@inproceedings{1020256,
  abstract     = {For high-throughput purposes, newly developed Fused-Core HPLC stationary phases (HALO® columns) have attracted the interest of the chromatographic community. Due to their small particle size (2.7 μm) and unique particle technology with 0.5 μm porous shell fused to a solid core particle (1.7 µm diameter), these columns create fast and high performance separations.
For our skin research, in vitro Franz diffusion cell (FDC) experiments are performed, resulting in large sample numbers of low concentrated bio-active in physiologic receptor media (e.g. PBS). Spilanthol, present in Spilanthes acmella as most prominent N-alkylamide and having promising transdermal activity [1, 2], could be analyzed in reversed-phase mode on the HALO® amide stationary phase with different mobile phases.
Several aspects are becoming more important with these fast HPLC columns compared to the conventional columns: injection volume, sample/mobile phase solvent strength, as well as detector/data intake. We demonstrate here that all these parameters are influencing the chromatographic behaviour, and should be well defined in the method description and validation.
Using Franz diffusion cells, the transdermal behaviour of spilanthol in HPMC-based patches with different percentages plasticizer (triethylcitrate (TEC)) and penetration enhancer (oleic acid (OA)) was investigated with the optimized Fused-Core method.
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, Journal of	Ethnopharmacology 127(1) (2010) 77-84.
[2]	J. Boonen, B. Baert, C. Burvenich, P. Blondeel, S. De Saeger, B. De Spiegeleer, LC–MS	profiling of N-alkylamides in Spilanthes acmella extract and the transmucosal behaviour of its	main bio-active spilanthol, Journal of Pharmaceutical and Biomedical Analysis (2010),	doi:10.1016/j.jpba.2010.02.010.},
  author       = {Boonen, Jente and De Spiegeleer, Bart},
  booktitle    = {Drug Analysis 2010, Abstracts},
  language     = {eng},
  location     = {Antwerp, Belgium},
  title        = {Amide fused-core chromatography of spilanthol as applied on a patch development},
  year         = {2010},
}