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Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies

Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which charac...

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Autores principales: Pena-Rodríguez, Eloy, Lajarin-Reinares, Maria, Mata-Ventosa, Aida, Pérez-Torras, Sandra, Fernández-Campos, Francisco
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8068797/
https://www.ncbi.nlm.nih.gov/pubmed/33920403
http://dx.doi.org/10.3390/pharmaceutics13040533
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author Pena-Rodríguez, Eloy
Lajarin-Reinares, Maria
Mata-Ventosa, Aida
Pérez-Torras, Sandra
Fernández-Campos, Francisco
author_facet Pena-Rodríguez, Eloy
Lajarin-Reinares, Maria
Mata-Ventosa, Aida
Pérez-Torras, Sandra
Fernández-Campos, Francisco
author_sort Pena-Rodríguez, Eloy
collection PubMed
description Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which characterization of their physicochemical properties was carried out. Dexamethasone was encapsulated in the lipomers (size, 115 nm; polydispersity, 0.24; zeta-potential (Z-potential), +30 mV) and their in vitro release profiles against dexamethasone in solution were investigated by vertical diffusion Franz cells. The skin biodistribution of the fluorescent-loaded lipomers was observed using confocal microscopy, demonstrating the accumulation of both lipomers and fluorochromes in the hair follicles of pig skin. To confirm this fact, immunofluorescence of the dexamethasone-loaded lipomers was carried out in pig hair follicles. The anti-inflammatory (via TNFα) efficacy of the dexamethasone-loaded lipomers was demonstrated in vitro in an HEK001 human keratinocytes cell culture and the in vitro cytotoxicity of the nanoformulation was investigated.
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spelling pubmed-80687972021-04-26 Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies Pena-Rodríguez, Eloy Lajarin-Reinares, Maria Mata-Ventosa, Aida Pérez-Torras, Sandra Fernández-Campos, Francisco Pharmaceutics Article Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which characterization of their physicochemical properties was carried out. Dexamethasone was encapsulated in the lipomers (size, 115 nm; polydispersity, 0.24; zeta-potential (Z-potential), +30 mV) and their in vitro release profiles against dexamethasone in solution were investigated by vertical diffusion Franz cells. The skin biodistribution of the fluorescent-loaded lipomers was observed using confocal microscopy, demonstrating the accumulation of both lipomers and fluorochromes in the hair follicles of pig skin. To confirm this fact, immunofluorescence of the dexamethasone-loaded lipomers was carried out in pig hair follicles. The anti-inflammatory (via TNFα) efficacy of the dexamethasone-loaded lipomers was demonstrated in vitro in an HEK001 human keratinocytes cell culture and the in vitro cytotoxicity of the nanoformulation was investigated. MDPI 2021-04-11 /pmc/articles/PMC8068797/ /pubmed/33920403 http://dx.doi.org/10.3390/pharmaceutics13040533 Text en © 2021 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
Pena-Rodríguez, Eloy
Lajarin-Reinares, Maria
Mata-Ventosa, Aida
Pérez-Torras, Sandra
Fernández-Campos, Francisco
Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies
title Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies
title_full Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies
title_fullStr Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies
title_full_unstemmed Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies
title_short Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies
title_sort dexamethasone-loaded lipomers: development, characterization, and skin biodistribution studies
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8068797/
https://www.ncbi.nlm.nih.gov/pubmed/33920403
http://dx.doi.org/10.3390/pharmaceutics13040533
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