Transdermal behaviour of the N-alkylamide spilanthol (affinin) from Spilanthes acmella (Compositae) extracts

被引:61
作者
Boonen, J. [1 ]
Baert, B. [1 ]
Roche, N. [2 ]
Burvenich, C. [3 ]
De Spiegeleer, Bart [1 ]
机构
[1] Univ Ghent, Drug Qual & Registrat Grp, Fac Pharmaceut Sci, Harelbekestr 72, B-9000 Ghent, Belgium
[2] Ghent Univ Hosp, Dept Plast & Reconstruct Surg, B-9000 Ghent, Belgium
[3] Univ Ghent, Fac Vet Med, Dept Physiol & Biometr, B-9820 Merelbeke, Belgium
关键词
Spilanthol (affinin); Human skin; Acmella; Transdermal; Franz diffusion cells; CAFFEIC ACID-DERIVATIVES; ECHINACEA-PURPUREA; HELIOPSIS-LONGIPES; SKIN PERMEATION; ENDOCANNABINOID SYSTEM; CHEMICAL-COMPOUNDS; MASS-SPECTROMETRY; DRUG-DELIVERY; ALKAMIDES; PHARMACOKINETICS;
D O I
10.1016/j.jep.2009.09.046
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Aim of the study: N-Alkylamides are a large group of bioactive molecules found in several plants from the genera Echinacea, Xanthoxylum and Spilanthes. Extracts and formulations derived from these plants are not only orally used, but also applied on the skin as well. However, there is currently 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. The present study investigates the transdermal behaviour of spilanthol, a prominent N-alkylamide. Materials and methods: Two pharmaceutically accepted dose solutions (ethanol and propylene glycol based aqueous donor vehicles), combined with three different receptor fluids (PBS, PBS + 0.5% HP beta CD, EtOH/H2O (30:70, v/v)), were applied on split-thickness human skin in a Franz diffusion cell (FDC) system. Fundamental permeation characteristics of spilanthol in a solvent-independent way (100% aqueous dose solution) were also obtained using an extrapolation approach with different organic solvent/H2O ratios. Results and conclusions: We demonstrated for the first time that spilanthol permeates the skin. The following aqueous-extrapolated primary transdermal parameters were obtained (mean SEM): K-p,K-aq = 3.31 (+/- 0.29) x 10(-3) cm/h. D-m,D-aq = 1.86 (+/- 0.09) x 10(-4) cm(2)/h and K-m,K-aq = 7.28 (+/- 1.59) x 10(-1). Partitioning (K-m) was strongly dependent on the donor solution composition, while diffusion (D-m) was mainly influenced by the receptor fluid composition. (C) 2009 Elsevier Ireland Ltd. All rights reserved.
引用
收藏
页码:77 / 84
页数:8
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