Cargando…

Pharmaceutical Development of Nanostructured Vesicular Hydrogel Formulations of Rifampicin for Wound Healing

Chronic wounds exhibit elevated levels of inflammatory cytokines, resulting in the release of proteolytic enzymes which delay wound-healing processes. In recent years, rifampicin has gained significant attention in the treatment of chronic wounds due to an interesting combination of antibacterial an...

Descripción completa

Detalles Bibliográficos
Autores principales: Wallenwein, Chantal M., Weigel, Verena, Hofhaus, Götz, Dhakal, Namrata, Schatton, Wolfgang, Gelperina, Svetlana, Groeber-Becker, Florian K., Dressman, Jennifer, Wacker, Matthias G.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9788359/
https://www.ncbi.nlm.nih.gov/pubmed/36555855
http://dx.doi.org/10.3390/ijms232416207
_version_ 1784858735242379264
author Wallenwein, Chantal M.
Weigel, Verena
Hofhaus, Götz
Dhakal, Namrata
Schatton, Wolfgang
Gelperina, Svetlana
Groeber-Becker, Florian K.
Dressman, Jennifer
Wacker, Matthias G.
author_facet Wallenwein, Chantal M.
Weigel, Verena
Hofhaus, Götz
Dhakal, Namrata
Schatton, Wolfgang
Gelperina, Svetlana
Groeber-Becker, Florian K.
Dressman, Jennifer
Wacker, Matthias G.
author_sort Wallenwein, Chantal M.
collection PubMed
description Chronic wounds exhibit elevated levels of inflammatory cytokines, resulting in the release of proteolytic enzymes which delay wound-healing processes. In recent years, rifampicin has gained significant attention in the treatment of chronic wounds due to an interesting combination of antibacterial and anti-inflammatory effects. Unfortunately, rifampicin is sensitive to hydrolysis and oxidation. As a result, no topical drug product for wound-healing applications has been approved. To address this medical need two nanostructured hydrogel formulations of rifampicin were developed. The liposomal vesicles were embedded into hydroxypropyl methylcellulose (HPMC) gel or a combination of hyaluronic acid and marine collagen. To protect rifampicin from degradation in aqueous environments, a freeze-drying method was developed. Before freeze-drying, two well-defined hydrogel preparations were obtained. After freeze-drying, the visual appearance, chemical stability, residual moisture content, and redispersion time of both preparations were within acceptable limits. However, the morphological characterization revealed an increase in the vesicle size for collagen–hyaluronic acid hydrogel. This was confirmed by subsequent release studies. Interactions of marine collagen with phosphatidylcholine were held responsible for this effect. The HPMC hydrogel formulation remained stable over 6 months of storage. Moving forward, this product fulfills all criteria to be evaluated in preclinical and clinical studies.
format Online
Article
Text
id pubmed-9788359
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-97883592022-12-24 Pharmaceutical Development of Nanostructured Vesicular Hydrogel Formulations of Rifampicin for Wound Healing Wallenwein, Chantal M. Weigel, Verena Hofhaus, Götz Dhakal, Namrata Schatton, Wolfgang Gelperina, Svetlana Groeber-Becker, Florian K. Dressman, Jennifer Wacker, Matthias G. Int J Mol Sci Article Chronic wounds exhibit elevated levels of inflammatory cytokines, resulting in the release of proteolytic enzymes which delay wound-healing processes. In recent years, rifampicin has gained significant attention in the treatment of chronic wounds due to an interesting combination of antibacterial and anti-inflammatory effects. Unfortunately, rifampicin is sensitive to hydrolysis and oxidation. As a result, no topical drug product for wound-healing applications has been approved. To address this medical need two nanostructured hydrogel formulations of rifampicin were developed. The liposomal vesicles were embedded into hydroxypropyl methylcellulose (HPMC) gel or a combination of hyaluronic acid and marine collagen. To protect rifampicin from degradation in aqueous environments, a freeze-drying method was developed. Before freeze-drying, two well-defined hydrogel preparations were obtained. After freeze-drying, the visual appearance, chemical stability, residual moisture content, and redispersion time of both preparations were within acceptable limits. However, the morphological characterization revealed an increase in the vesicle size for collagen–hyaluronic acid hydrogel. This was confirmed by subsequent release studies. Interactions of marine collagen with phosphatidylcholine were held responsible for this effect. The HPMC hydrogel formulation remained stable over 6 months of storage. Moving forward, this product fulfills all criteria to be evaluated in preclinical and clinical studies. MDPI 2022-12-19 /pmc/articles/PMC9788359/ /pubmed/36555855 http://dx.doi.org/10.3390/ijms232416207 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
Wallenwein, Chantal M.
Weigel, Verena
Hofhaus, Götz
Dhakal, Namrata
Schatton, Wolfgang
Gelperina, Svetlana
Groeber-Becker, Florian K.
Dressman, Jennifer
Wacker, Matthias G.
Pharmaceutical Development of Nanostructured Vesicular Hydrogel Formulations of Rifampicin for Wound Healing
title Pharmaceutical Development of Nanostructured Vesicular Hydrogel Formulations of Rifampicin for Wound Healing
title_full Pharmaceutical Development of Nanostructured Vesicular Hydrogel Formulations of Rifampicin for Wound Healing
title_fullStr Pharmaceutical Development of Nanostructured Vesicular Hydrogel Formulations of Rifampicin for Wound Healing
title_full_unstemmed Pharmaceutical Development of Nanostructured Vesicular Hydrogel Formulations of Rifampicin for Wound Healing
title_short Pharmaceutical Development of Nanostructured Vesicular Hydrogel Formulations of Rifampicin for Wound Healing
title_sort pharmaceutical development of nanostructured vesicular hydrogel formulations of rifampicin for wound healing
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9788359/
https://www.ncbi.nlm.nih.gov/pubmed/36555855
http://dx.doi.org/10.3390/ijms232416207
work_keys_str_mv AT wallenweinchantalm pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing
AT weigelverena pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing
AT hofhausgotz pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing
AT dhakalnamrata pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing
AT schattonwolfgang pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing
AT gelperinasvetlana pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing
AT groeberbeckerfloriank pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing
AT dressmanjennifer pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing
AT wackermatthiasg pharmaceuticaldevelopmentofnanostructuredvesicularhydrogelformulationsofrifampicinforwoundhealing