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

We demonstrated the anti-inflammatory and anti-oxidative effects of <i>Humulus lupulus</i> (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 topicall...

Full description

Bibliographic Details
Main Authors: Zita Hurth, Marie-Luise Faber, Fabian Gendrisch, Martin Holzer, Birgit Haarhaus, Anja Cawelius, Kay Schwabe, Christoph Mathis Schempp, Ute Wölfle
Format: Article
Language:English
Published: MDPI AG 2022-03-01
Series:Pharmaceuticals
Subjects:
Online Access:https://www.mdpi.com/1424-8247/15/3/350
_version_ 1797443726371454976
author Zita Hurth
Marie-Luise Faber
Fabian Gendrisch
Martin Holzer
Birgit Haarhaus
Anja Cawelius
Kay Schwabe
Christoph Mathis Schempp
Ute Wölfle
author_facet Zita Hurth
Marie-Luise Faber
Fabian Gendrisch
Martin Holzer
Birgit Haarhaus
Anja Cawelius
Kay Schwabe
Christoph Mathis Schempp
Ute Wölfle
author_sort Zita Hurth
collection DOAJ
description We demonstrated the anti-inflammatory and anti-oxidative effects of <i>Humulus lupulus</i> (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.
first_indexed 2024-03-09T13:01:14Z
format Article
id doaj.art-d9ff24d9f2b04485b729e1351f31868b
institution Directory Open Access Journal
issn 1424-8247
language English
last_indexed 2024-03-09T13:01:14Z
publishDate 2022-03-01
publisher MDPI AG
record_format Article
series Pharmaceuticals
spelling doaj.art-d9ff24d9f2b04485b729e1351f31868b2023-11-30T21:54:52ZengMDPI AGPharmaceuticals1424-82472022-03-0115335010.3390/ph15030350The Anti-Inflammatory Effect of <i>Humulus lupulus</i> Extract In Vivo Depends on the Galenic System of the Topical FormulationZita Hurth0Marie-Luise Faber1Fabian Gendrisch2Martin Holzer3Birgit Haarhaus4Anja Cawelius5Kay Schwabe6Christoph Mathis Schempp7Ute Wölfle8Research Center Skinitial, Department of Dermatology, Medical Center, University of Freiburg, Faculty of Medicine, University of Freiburg, 79106 Freiburg, GermanyResearch Center Skinitial, Department of Dermatology, Medical Center, University of Freiburg, Faculty of Medicine, University of Freiburg, 79106 Freiburg, GermanyResearch Center Skinitial, Department of Dermatology, Medical Center, University of Freiburg, Faculty of Medicine, University of Freiburg, 79106 Freiburg, GermanyDepartment of Pharmaceutical Technology and Biopharmacy, Institute of Pharmaceutical Sciences, Faculty of Chemistry and Pharmacy, University of Freiburg, 79104 Freiburg, GermanyResearch Center Skinitial, Department of Dermatology, Medical Center, University of Freiburg, Faculty of Medicine, University of Freiburg, 79106 Freiburg, GermanyFlavex Naturextrakte GmbH, 66780 Rehlingen, GermanyBSI-Beauty Science Intelligence GmbH, 30855 Langenhagen, GermanyResearch Center Skinitial, Department of Dermatology, Medical Center, University of Freiburg, Faculty of Medicine, University of Freiburg, 79106 Freiburg, GermanyResearch Center Skinitial, Department of Dermatology, Medical Center, University of Freiburg, Faculty of Medicine, University of Freiburg, 79106 Freiburg, GermanyWe demonstrated the anti-inflammatory and anti-oxidative effects of <i>Humulus lupulus</i> (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.https://www.mdpi.com/1424-8247/15/3/350<i>Humulus lupulus</i>Franz diffusion cellsUVB erythema test
spellingShingle Zita Hurth
Marie-Luise Faber
Fabian Gendrisch
Martin Holzer
Birgit Haarhaus
Anja Cawelius
Kay Schwabe
Christoph Mathis Schempp
Ute Wölfle
The Anti-Inflammatory Effect of <i>Humulus lupulus</i> Extract In Vivo Depends on the Galenic System of the Topical Formulation
Pharmaceuticals
<i>Humulus lupulus</i>
Franz diffusion cells
UVB erythema test
title The Anti-Inflammatory Effect of <i>Humulus lupulus</i> Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_full The Anti-Inflammatory Effect of <i>Humulus lupulus</i> Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_fullStr The Anti-Inflammatory Effect of <i>Humulus lupulus</i> Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_full_unstemmed The Anti-Inflammatory Effect of <i>Humulus lupulus</i> Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_short The Anti-Inflammatory Effect of <i>Humulus lupulus</i> Extract In Vivo Depends on the Galenic System of the Topical Formulation
title_sort anti inflammatory effect of i humulus lupulus i extract in vivo depends on the galenic system of the topical formulation
topic <i>Humulus lupulus</i>
Franz diffusion cells
UVB erythema test
url https://www.mdpi.com/1424-8247/15/3/350
work_keys_str_mv AT zitahurth theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT marieluisefaber theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT fabiangendrisch theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT martinholzer theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT birgithaarhaus theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT anjacawelius theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT kayschwabe theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT christophmathisschempp theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT utewolfle theantiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT zitahurth antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT marieluisefaber antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT fabiangendrisch antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT martinholzer antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT birgithaarhaus antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT anjacawelius antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT kayschwabe antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT christophmathisschempp antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation
AT utewolfle antiinflammatoryeffectofihumuluslupulusiextractinvivodependsonthegalenicsystemofthetopicalformulation