Skin penetration enhancing properties of the plant N-alkylamide spilanthol

Spiegeleer, Bart De; Boonen, Jente; Malysheva, Svetlana V.; Mavungu, José Diana Di; Saeger, Sarah De; Roche, Nathalie; Blondeel, Phillip; Taevernier, Lien; Veryser, Lieselotte

doi:10.1016/j.jep.2013.03.076

Cited by 37 publications

(32 citation statements)

References 29 publications

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“…The experimentally determined K p of the negative control (2.05 × 10 -3 cm/h) is comparable with our previous result (2.19 × 10 -3 cm/h) [15]. The distribution of ibuprofen into the different skin layers is given in figure 8.…”

Section: Resultssupporting

confidence: 88%

“…The experimentally determined K p of the negative control, i.e. caffeine without any PCER (2.11·10 -4 cm/h), is comparable with our previous result (2.23·10 -4 cm/h) [15]. The highest K p values of all the PCERs were seen with PCER2, PCER3 and PCER6.…”

Section: Resultssupporting

confidence: 88%

“…The experimentally determined K p of the negative control (3.92 × 10 -4 cm/h) is almost the same as our previous result (3.97 × 10 -4 cm/h) [15]. There is no clear trend noticeable between high partition coefficient values of testosterone and the ratio…”

Section: Resultssupporting

confidence: 88%

“…A mobile phase composition of 75/25 A/B (% V/V) was used for the determination of caffeine and ibuprofen, while a 30/70 A/B (% V/V) composition was used for the testosterone determination. UV detection was performed at 272, 254 and 220 nm for caffeine, testosterone and ibuprofen, respectively, with peak areas used for quantification [15]. …”

Section: Methodsmentioning

confidence: 99%

“…The well-known penetration enhancer azone served as a positive control. In our previous studies, these model compounds were already investigated in the presence or absence of other penetration enhancers, such as spilanthol [15,16]. …”

Section: Introductionmentioning

confidence: 99%

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The Influence of the Acyl Chain on the Transdermal Penetration-Enhancing Effect of Synthetic Phytoceramides

Veryser¹,

Boonen²,

Taevernier³

et al. 2014

Skin Pharmacol Physiol

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Background/Aims: The skin has become very attractive as a route for drug administration. Optimization of topical drug formulations by the addition of penetration enhancers may facilitate the passage of drugs through the stratum corneum. Methods: In this paper, the skin penetration effect of phytosphingosine and 9 derived phytoceramides (PCERs) on 3 transdermal model drugs (i.e. caffeine, testosterone, ibuprofen) was investigated via Franz diffusion cell experiments using split-thickness human skin. Azone was included as a positive control. Results: The main finding in our study was that the PCERs exerted a compound-dependent penetration-enhancing effect. Some of the investigated PCERs exhibited a penetration-enhancing ratio of more than 2 (mean ± SE): for caffeine PCER1 (2.48 ± 0.44), PCER2 (2.75 ± 0.74), PCER3 (2.62 ± 0.93) and PCER6 (2.70 ± 0.45) and for testosterone PCER1 (2.08 ± 0.56), PCER2 (2.56 ± 0.13), PCER3 (3.48), PCER4 (2.53), PCER5 (2.04 ± 0.14), PCER6 (2.05 ± 0.48) and PCER10 (4.84 ± 0.79), but none of them had an influence on ibuprofen. Conclusion: The investigated PCERs exhibited a penetration-enhancing effect on caffeine and testosterone but not on ibuprofen.

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Section: Resultssupporting

confidence: 88%

Section: Resultssupporting

confidence: 88%

Section: Resultssupporting

confidence: 88%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

The Influence of the Acyl Chain on the Transdermal Penetration-Enhancing Effect of Synthetic Phytoceramides

Veryser¹,

Boonen²,

Taevernier³

et al. 2014

Skin Pharmacol Physiol

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Investigation of the in-vitro lethal effect of spilanthol on demodex and finding the most effective dose

Kara,

Dikicier,

Solak

et al. 2024

Arch Dermatol Res

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Acaricide activity in vitro of Acmella oleracea against Rhipicephalus microplus

Castro

Lima²,

Vasconcelos³

et al. 2014

Parasitol Res

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Cattle tick control has been limited by the resistance of these parasites to synthetic acaricides. Natural products are a possible alternative as they have different mechanisms of action. Acmella oleracea is a native plant with a large cultivated area in the Amazon region and could be easily used for large-scale preparation of a commercial product. This study evaluated the in vitro action of the hexane extract of the aerial parts of A. oleracea on larvae and engorged females of the cattle tick Rhipicephalus microplus. Spilanthol was the major constituent with a content of 14.8% in the extract. The hexane extract of A. oleracea was highly effective against larvae of R. microplus with an LC50 of 0.8 mg mL(-1). Against engorged females, hexane extract of A. oleracea reduced oviposition and hatchability of eggs with an LC50 of 79.7 mg mL(-1). Larvae and engorged females were killed by the hexane extract with high efficiency (>95%) at concentrations of 3.1 and 150.0 mg mL(-1), respectively. These results demonstrate that the hexane extract of A. oleracea has significant activity against R. microplus and has potential to be developed into formulations for tick control.

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Skin penetration enhancing properties of the plant N-alkylamide spilanthol

Cited by 37 publications

References 29 publications

The Influence of the Acyl Chain on the Transdermal Penetration-Enhancing Effect of Synthetic Phytoceramides

The Influence of the Acyl Chain on the Transdermal Penetration-Enhancing Effect of Synthetic Phytoceramides

Investigation of the in-vitro lethal effect of spilanthol on demodex and finding the most effective dose

Acaricide activity in vitro of Acmella oleracea against Rhipicephalus microplus

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