Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture
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 es...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-03-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/4/742 |
| _version_ | 1827627163377991680 |
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| author | Franziska M. Jürgens Fabian C. Herrmann Sara M. Robledo Thomas J. Schmidt |
| author_facet | Franziska M. Jürgens Fabian C. Herrmann Sara M. Robledo Thomas J. Schmidt |
| author_sort | Franziska M. Jürgens |
| collection | DOAJ |
| description | 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<sup>−2</sup>·h<sup>−1</sup>) and the more permeable human skin B (TEWL = 17.271 g·m<sup>−2</sup>·h<sup>−1</sup>), 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. |
| first_indexed | 2024-03-09T13:09:31Z |
| format | Article |
| id | doaj.art-4d1f51f8617548feafce7a563f0db3ec |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T13:09:31Z |
| publishDate | 2022-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-4d1f51f8617548feafce7a563f0db3ec2023-11-30T21:43:50ZengMDPI AGPharmaceutics1999-49232022-03-0114474210.3390/pharmaceutics14040742Dermal Absorption of Sesquiterpene Lactones from Arnica TinctureFranziska M. Jürgens0Fabian C. Herrmann1Sara M. Robledo2Thomas J. Schmidt3Institute of Pharmaceutical Biology and Phytochemistry, University of Münster, PharmaCampus, Corrensstrasse 48, D-48149 Münster, GermanyInstitute of Pharmaceutical Biology and Phytochemistry, University of Münster, PharmaCampus, Corrensstrasse 48, D-48149 Münster, GermanyPECET-School of Medicine, University of Antioquia, Calle 70 # 52-21, Medellin 0500100, ColombiaInstitute of Pharmaceutical Biology and Phytochemistry, University of Münster, PharmaCampus, Corrensstrasse 48, D-48149 Münster, GermanyArnica 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<sup>−2</sup>·h<sup>−1</sup>) and the more permeable human skin B (TEWL = 17.271 g·m<sup>−2</sup>·h<sup>−1</sup>), 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.https://www.mdpi.com/1999-4923/14/4/742Arnica tincturesesquiterpene lactoneshelenalinnatural productsdermal absorptionskin penetration |
| spellingShingle | Franziska M. Jürgens Fabian C. Herrmann Sara M. Robledo Thomas J. Schmidt Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture Pharmaceutics Arnica tincture sesquiterpene lactones helenalin natural products dermal absorption skin penetration |
| title | Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture |
| title_full | Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture |
| title_fullStr | Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture |
| title_full_unstemmed | Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture |
| title_short | Dermal Absorption of Sesquiterpene Lactones from Arnica Tincture |
| title_sort | dermal absorption of sesquiterpene lactones from arnica tincture |
| topic | Arnica tincture sesquiterpene lactones helenalin natural products dermal absorption skin penetration |
| url | https://www.mdpi.com/1999-4923/14/4/742 |
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