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Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies

This work evaluated the occlusive versus non-occlusive application of microemulsion (ME) for the transdermal delivery of progesterone. The mechanisms of enhanced skin penetration were investigated. ME comprised of oleic acid, Tween 80, propylene glycol, and water, was used neat or with ethanol as a...

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Autor principal: El Maghraby, Gamal M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Österreichische Apotheker-Verlagsgesellschaft 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3447611/
https://www.ncbi.nlm.nih.gov/pubmed/23008820
http://dx.doi.org/10.3797/scipharm.1201-01
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author El Maghraby, Gamal M.
author_facet El Maghraby, Gamal M.
author_sort El Maghraby, Gamal M.
collection PubMed
description This work evaluated the occlusive versus non-occlusive application of microemulsion (ME) for the transdermal delivery of progesterone. The mechanisms of enhanced skin penetration were investigated. ME comprised of oleic acid, Tween 80, propylene glycol, and water, was used neat or with ethanol as a volatile cosurfactant. The ME formulations enhanced progesterone transdermal flux compared to the saturated drug solution in 14% aqueous propylene glycol (control). Ethanol-containing ME (EME) was better than the ethanol-free system (EFME). Open application of EFME produced a marginal reduction in flux compared to occlusive application. For EME, open application reduced the flux by 26–28% with the flux remaining significantly higher than that obtained with EFME. The mechanistic studies revealed synergism between ethanol and EFME with EME, producing greater flux than the sum of fluxes obtained from 40% ethanol in water and EFME. Penetration enhancement and supersaturation played a role in enhanced transdermal delivery, but other mechanisms were also possible. This study thus introduced EME as a transdermal delivery system for progesterone with good potential for open application as a spray.
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spelling pubmed-34476112012-09-24 Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies El Maghraby, Gamal M. Sci Pharm Research Article This work evaluated the occlusive versus non-occlusive application of microemulsion (ME) for the transdermal delivery of progesterone. The mechanisms of enhanced skin penetration were investigated. ME comprised of oleic acid, Tween 80, propylene glycol, and water, was used neat or with ethanol as a volatile cosurfactant. The ME formulations enhanced progesterone transdermal flux compared to the saturated drug solution in 14% aqueous propylene glycol (control). Ethanol-containing ME (EME) was better than the ethanol-free system (EFME). Open application of EFME produced a marginal reduction in flux compared to occlusive application. For EME, open application reduced the flux by 26–28% with the flux remaining significantly higher than that obtained with EFME. The mechanistic studies revealed synergism between ethanol and EFME with EME, producing greater flux than the sum of fluxes obtained from 40% ethanol in water and EFME. Penetration enhancement and supersaturation played a role in enhanced transdermal delivery, but other mechanisms were also possible. This study thus introduced EME as a transdermal delivery system for progesterone with good potential for open application as a spray. Österreichische Apotheker-Verlagsgesellschaft 2012 2012-06-18 /pmc/articles/PMC3447611/ /pubmed/23008820 http://dx.doi.org/10.3797/scipharm.1201-01 Text en © El Maghraby; licensee Österreichische Apotheker-Verlagsgesellschaft m. b. H., Vienna, Austria. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/3.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
El Maghraby, Gamal M.
Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies
title Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies
title_full Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies
title_fullStr Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies
title_full_unstemmed Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies
title_short Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies
title_sort occlusive and non-occlusive application of microemulsion for transdermal delivery of progesterone: mechanistic studies
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3447611/
https://www.ncbi.nlm.nih.gov/pubmed/23008820
http://dx.doi.org/10.3797/scipharm.1201-01
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