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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...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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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. |
format | Online Article Text |
id | pubmed-8308946 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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