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In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers

Lipid nanoparticles (LNPs) have been proposed as carriers for drug skin delivery and targeting. As LNPs effectiveness could be increased by the addition of chemical penetration enhancers (PE), in this work, the feasibility of incorporating PE into LNPs to improve idebenone (IDE) targeting to the ski...

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Autores principales: Montenegro, Lucia, Santagati, Ludovica Maria, Sarpietro, Maria Grazia, Castelli, Francesco, Panico, Annamaria, Siciliano, Edy Angela, Lai, Francesco, Valenti, Donatella, Sinico, Chiara
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8308946/
https://www.ncbi.nlm.nih.gov/pubmed/34371719
http://dx.doi.org/10.3390/pharmaceutics13071027
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author Montenegro, Lucia
Santagati, Ludovica Maria
Sarpietro, Maria Grazia
Castelli, Francesco
Panico, Annamaria
Siciliano, Edy Angela
Lai, Francesco
Valenti, Donatella
Sinico, Chiara
author_facet Montenegro, Lucia
Santagati, Ludovica Maria
Sarpietro, Maria Grazia
Castelli, Francesco
Panico, Annamaria
Siciliano, Edy Angela
Lai, Francesco
Valenti, Donatella
Sinico, Chiara
author_sort Montenegro, Lucia
collection PubMed
description Lipid nanoparticles (LNPs) have been proposed as carriers for drug skin delivery and targeting. As LNPs effectiveness could be increased by the addition of chemical penetration enhancers (PE), in this work, the feasibility of incorporating PE into LNPs to improve idebenone (IDE) targeting to the skin was investigated. LNPs loading IDE 0.7% w/w were prepared using hydrophilic (propylene glycol, PG, 10% w/w or N-methylpyrrolidone, NMP, 10% w/w) and/or lipophilic PE (oleic acid, OA, 1% w/w; isopropyl myristate, IPM, 3.5% w/w; a mixture of 0.5% w/w OA and 2.5% w/w IPM). All LNPs showed small sizes (<60 nm), low polydispersity index and good stability. According to the obtained results, IDE release from LNPs was not the rate-limiting step in IDE skin penetration. No IDE permeation was observed through excised pigskin from all LNPs, while the greatest increase of IDE penetration into the different skin layers was obtained using the mixture OA/IPM. The antioxidant activity of IDE-loaded LNPs, determined by the oxygen radical absorbance capacity assay, was greater than that of free IDE. These results suggest that the use of suitable PE as LNPs components could be regarded as a promising strategy to improve drug targeting to the skin.
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spelling pubmed-83089462021-07-25 In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers Montenegro, Lucia Santagati, Ludovica Maria Sarpietro, Maria Grazia Castelli, Francesco Panico, Annamaria Siciliano, Edy Angela Lai, Francesco Valenti, Donatella Sinico, Chiara Pharmaceutics Article Lipid nanoparticles (LNPs) have been proposed as carriers for drug skin delivery and targeting. As LNPs effectiveness could be increased by the addition of chemical penetration enhancers (PE), in this work, the feasibility of incorporating PE into LNPs to improve idebenone (IDE) targeting to the skin was investigated. LNPs loading IDE 0.7% w/w were prepared using hydrophilic (propylene glycol, PG, 10% w/w or N-methylpyrrolidone, NMP, 10% w/w) and/or lipophilic PE (oleic acid, OA, 1% w/w; isopropyl myristate, IPM, 3.5% w/w; a mixture of 0.5% w/w OA and 2.5% w/w IPM). All LNPs showed small sizes (<60 nm), low polydispersity index and good stability. According to the obtained results, IDE release from LNPs was not the rate-limiting step in IDE skin penetration. No IDE permeation was observed through excised pigskin from all LNPs, while the greatest increase of IDE penetration into the different skin layers was obtained using the mixture OA/IPM. The antioxidant activity of IDE-loaded LNPs, determined by the oxygen radical absorbance capacity assay, was greater than that of free IDE. These results suggest that the use of suitable PE as LNPs components could be regarded as a promising strategy to improve drug targeting to the skin. MDPI 2021-07-06 /pmc/articles/PMC8308946/ /pubmed/34371719 http://dx.doi.org/10.3390/pharmaceutics13071027 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
Montenegro, Lucia
Santagati, Ludovica Maria
Sarpietro, Maria Grazia
Castelli, Francesco
Panico, Annamaria
Siciliano, Edy Angela
Lai, Francesco
Valenti, Donatella
Sinico, Chiara
In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers
title In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers
title_full In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers
title_fullStr In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers
title_full_unstemmed In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers
title_short In Vitro Skin Permeation of Idebenone from Lipid Nanoparticles Containing Chemical Penetration Enhancers
title_sort in vitro skin permeation of idebenone from lipid nanoparticles containing chemical penetration enhancers
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8308946/
https://www.ncbi.nlm.nih.gov/pubmed/34371719
http://dx.doi.org/10.3390/pharmaceutics13071027
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