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The Anti-Inflammatory Effect of Humulus lupulus Extract In Vivo Depends on the Galenic System of the Topical Formulation

We demonstrated the anti-inflammatory and anti-oxidative effects of Humulus lupulus (HL) extract on solar simulator-irradiated primary human keratinocytes (PHKs) by analyzing ERK and p38 MAPK phosphorylation and production of IL-6 and IL-8. The anti-inflammatory effect of topically applied HL was fu...

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Autores principales: Hurth, Zita, Faber, Marie-Luise, Gendrisch, Fabian, Holzer, Martin, Haarhaus, Birgit, Cawelius, Anja, Schwabe, Kay, Schempp, Christoph Mathis, Wölfle, Ute
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8951350/
https://www.ncbi.nlm.nih.gov/pubmed/35337147
http://dx.doi.org/10.3390/ph15030350
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author Hurth, Zita
Faber, Marie-Luise
Gendrisch, Fabian
Holzer, Martin
Haarhaus, Birgit
Cawelius, Anja
Schwabe, Kay
Schempp, Christoph Mathis
Wölfle, Ute
author_facet Hurth, Zita
Faber, Marie-Luise
Gendrisch, Fabian
Holzer, Martin
Haarhaus, Birgit
Cawelius, Anja
Schwabe, Kay
Schempp, Christoph Mathis
Wölfle, Ute
author_sort Hurth, Zita
collection PubMed
description We demonstrated the anti-inflammatory and anti-oxidative effects of Humulus lupulus (HL) extract on solar simulator-irradiated primary human keratinocytes (PHKs) by analyzing ERK and p38 MAPK phosphorylation and production of IL-6 and IL-8. The anti-inflammatory effect of topically applied HL was further tested in vivo on human skin. To this end, we developed an oil-in-water (O/W) and a water-in-oil (W/O) cream with a lipid content of 40%. The anti-inflammatory effect of 1% HL extract incorporated in these two vehicles was assessed in a randomized, prospective, placebo controlled, double-blind UVB erythema study with 40 healthy volunteers. Hydrocortisone acetate (HCA) in the corresponding vehicle served as positive control. Surprisingly, both HL and HCA were only effective in the O/W system but not in the W/O formulation. Release studies using vertical diffusion cells (Franz cells) revealed that HCA was released in much higher amounts from the O/W cream compared to the W/O formulation. In summary, we have shown that 1% HL extract exerts anti-inflammatory effects comparable to 1% HCA, but only when incorporated in our O/W cream. Our findings confirm the critical role of the vehicle in topical anti-inflammatory systems.
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spelling pubmed-89513502022-03-26 The Anti-Inflammatory Effect of Humulus lupulus Extract In Vivo Depends on the Galenic System of the Topical Formulation Hurth, Zita Faber, Marie-Luise Gendrisch, Fabian Holzer, Martin Haarhaus, Birgit Cawelius, Anja Schwabe, Kay Schempp, Christoph Mathis Wölfle, Ute Pharmaceuticals (Basel) Article We demonstrated the anti-inflammatory and anti-oxidative effects of Humulus lupulus (HL) extract on solar simulator-irradiated primary human keratinocytes (PHKs) by analyzing ERK and p38 MAPK phosphorylation and production of IL-6 and IL-8. The anti-inflammatory effect of topically applied HL was further tested in vivo on human skin. To this end, we developed an oil-in-water (O/W) and a water-in-oil (W/O) cream with a lipid content of 40%. The anti-inflammatory effect of 1% HL extract incorporated in these two vehicles was assessed in a randomized, prospective, placebo controlled, double-blind UVB erythema study with 40 healthy volunteers. Hydrocortisone acetate (HCA) in the corresponding vehicle served as positive control. Surprisingly, both HL and HCA were only effective in the O/W system but not in the W/O formulation. Release studies using vertical diffusion cells (Franz cells) revealed that HCA was released in much higher amounts from the O/W cream compared to the W/O formulation. In summary, we have shown that 1% HL extract exerts anti-inflammatory effects comparable to 1% HCA, but only when incorporated in our O/W cream. Our findings confirm the critical role of the vehicle in topical anti-inflammatory systems. MDPI 2022-03-14 /pmc/articles/PMC8951350/ /pubmed/35337147 http://dx.doi.org/10.3390/ph15030350 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Hurth, Zita
Faber, Marie-Luise
Gendrisch, Fabian
Holzer, Martin
Haarhaus, Birgit
Cawelius, Anja
Schwabe, Kay
Schempp, Christoph Mathis
Wölfle, Ute
The Anti-Inflammatory Effect of Humulus lupulus Extract In Vivo Depends on the Galenic System of the Topical Formulation
title The Anti-Inflammatory Effect of Humulus lupulus Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_full The Anti-Inflammatory Effect of Humulus lupulus Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_fullStr The Anti-Inflammatory Effect of Humulus lupulus Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_full_unstemmed The Anti-Inflammatory Effect of Humulus lupulus Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_short The Anti-Inflammatory Effect of Humulus lupulus Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_sort anti-inflammatory effect of humulus lupulus extract in vivo depends on the galenic system of the topical formulation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8951350/
https://www.ncbi.nlm.nih.gov/pubmed/35337147
http://dx.doi.org/10.3390/ph15030350
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