TY  - JOUR
AB  - Arnica tincture is a traditional herbal medicine used to treat blunt injuries, e.g., bruises and squeezes. In addition, a potential new use in the treatment of cutaneous leishmaniasis is currently under investigation. Therefore, detailed information about the dermal absorption of the tincture and especially its bioactive constituents, sesquiterpene lactones (STLs) of the helenalin- and 11α,13-dihydrohelenalin type, is mandatory. Consequently, this article reports on dermal absorption studies of Arnica tincture using diffusion cells and porcine skin as well as two human skin samples with different permeability. The amounts of STLs on the skin surfaces, in skin extracts and in the receptor fluids were quantified by ultra-high-performance liquid chromatography with high-resolution mass spectrometry (UHPLC-HRMS). It was found that Arnica STLs permeated into the receptor fluid already 4 h after the application, but the amount was rather low. Within 48 h, a maximum of 8.4%, 14.6% and 36.4% of STLs permeated through porcine skin, human skin A (trans-epidermal water loss (TEWL) = 11.518 g·m−2·h−1) and the more permeable human skin B (TEWL = 17.271 g·m−2·h−1), respectively. The majority of STLs was absorbed (penetrated into the skin; 97.6%, 97.8% and 99.3%) after 48 h but a huge portion could not be extracted from skin and is expected to be irreversibly bound to skin proteins. To better visualize the analytes in different skin layers, a fluorescence-labeled STL, helenalin 3,4-dimethoxycinnamate, was synthesized. Fluorescence microscopic images depict an accumulation of the fluorescent derivative in the epidermis. For the treatment of local, cutaneous complaints, an enrichment of the bioactive substances in the skin may be considered beneficial.
AU  - Jürgens, Franziska M.
AU  - Herrmann, Fabian C.
AU  - Herrmann, Fabian Christopher
AU  - Robledo, Sara M.
AU  - Schmidt, Thomas J.
DA  - 2022-03-29
DO  - 10.17879/14029399676
KW  - Arnica tincture
KW  - sesquiterpene lactones
KW  - helenalin
KW  - natural products
KW  - dermal absorption
KW  - skin penetration
KW  - diffusion cells
KW  - fluorescence microscopy
LA  - eng
N1  - Pharmaceutics 14 (2022) 4, 742, 1-17
N1  - Finanziert durch den Open-Access-Publikationsfonds der Westfälischen Wilhelms-Universität Münster (WWU Münster).
N1  - This research was funded by the Wilhelm Doerenkamp-Foundation, grant specification: NATVANTAGE RESEARCH GRANT 2018.
PY  - 2022-03-29
TI  - Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture
UR  - https://nbn-resolving.org/urn:nbn:de:hbz:6-14029398850
Y2  - 2024-11-21T19:21:24
ER  -