Permeation kinetics of active drugs through lanolin-based artificial membranes

Skin-penetration studies play an essential role in the selection of drugs for dermal or transdermal application. In vivo experiments in humans are not always possible for ethical, practical, or economic reasons, especially in the first part of the drug development. It is necessary to develop alterna...

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Autores: Alonso, Cristina, Collini, Ilaria, Carrer, Víctor, Barba, Clara, Martí, Meritxell, Coderch Negra, M. Luisa
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2020
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/212237
Acceso en línea:http://hdl.handle.net/10261/212237
Access Level:acceso abierto
Palabra clave:Synthetic membranes
Lanolin
Franz cells
Permeation profile
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spelling Permeation kinetics of active drugs through lanolin-based artificial membranesAlonso, CristinaCollini, IlariaCarrer, VíctorBarba, ClaraMartí, MeritxellCoderch Negra, M. LuisaSynthetic membranesLanolinFranz cellsPermeation profileSkin-penetration studies play an essential role in the selection of drugs for dermal or transdermal application. In vivo experiments in humans are not always possible for ethical, practical, or economic reasons, especially in the first part of the drug development. It is necessary to develop alternative methods using accessible and reproducible surrogates for in vivo human skin. The in vitro methodologies using biological membranes (human and animal skin) are recognized and well accepted as an alternative but present high inter- and intra-individual variability. Therefore, the formation of synthetic membranes has been studied to obtain skin- mimicking models for permeation studies. The aim of this work is to create lanolin-based artificial membranes that can mimic the absorption through the skin of compounds applied topically. A series of synthetic membranes using two different types of lanolin (water-extracted (WE) and solvent-extracted (SE)) were prepared. Next, the in vitro release test of three drugs (diclofenac sodium, ibuprofen and lidocaine) was performed on artificial membranes and on porcine skin placed on Franz cells. The percentage of release, flux, permeability coefficient, lag time, area under the curve, maximal concentration and time were determined for each compound in the different types of membrane. The results showed that lanolin membranes presented a strong diminution of permeability compared to most artificial membranes, leading to a very similar permeability to that of skin. The SE and WE membranes showed a diminution of transepidermal water loss and permeability of compounds compared with membranes alone. The results from WE membranes were similar to those found for the skin. The lanolin membranes were not capable of perfectly mimicking permeation through the skin, but they did have the same rank order of drug penetration as the skin. It may be deduced from these tests that these systems provide more reliable results for compounds with low to medium lipophilicity. The results demonstrated that new lanolin-based artificial membranes have the potential to be exploited as screening models for determining the permeability of a compound destined to be topically delivered.The present work could not be performed without the collaboration and contribution of the Service of Dermocosmetic Assessment from IQAC-CSIC. The authors are also grateful to Montserrat Rigol Muxart and Núria Solanes Batlló from the Department of Cardiology (Institut d’Investigacions Biomèdiques August Pi I Sunyer (IDIBAPS) Hospital Clínic, Universitat de Barcelona, Spain) for supplying the porcine skin biopsies. This work was supported by Ministerio de Ciencia, Innovación y Universidades, España (number CTQ2018-094014-B-100). The authors acknowledge also the Lifeprogram for financial support of the WDS “Eco-Efficient dry wool scouring with the total by-products recovery” LIFE 11 ENV/ES/588, Recuperación de Materiales Textiles (RMT) and Textile Manuel Tavares for providingthe lanolins.Peer reviewedElsevierBarba, Clara [0000-0002-3084-2925]Martí, Meritxell [0000-0001-9681-6466]Consejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]202020202020info:eu-repo/semantics/articlehttp://purl.org/coar/resource_type/c_6501Postprintinfo:eu-repo/semantics/acceptedVersionhttp://hdl.handle.net/10261/212237reponame:DIGITAL.CSIC. Repositorio Institucional del CSICinstname:Consejo Superior de Investigaciones Científicas (CSIC)Ingléshttps://doi.org/10.1016/j.colsurfb.2020.111024Síinfo:eu-repo/semantics/openAccessoai:digital.csic.es:10261/2122372026-05-22T06:33:51Z
dc.title.none.fl_str_mv Permeation kinetics of active drugs through lanolin-based artificial membranes
title Permeation kinetics of active drugs through lanolin-based artificial membranes
spellingShingle Permeation kinetics of active drugs through lanolin-based artificial membranes
Alonso, Cristina
Synthetic membranes
Lanolin
Franz cells
Permeation profile
title_short Permeation kinetics of active drugs through lanolin-based artificial membranes
title_full Permeation kinetics of active drugs through lanolin-based artificial membranes
title_fullStr Permeation kinetics of active drugs through lanolin-based artificial membranes
title_full_unstemmed Permeation kinetics of active drugs through lanolin-based artificial membranes
title_sort Permeation kinetics of active drugs through lanolin-based artificial membranes
dc.creator.none.fl_str_mv Alonso, Cristina
Collini, Ilaria
Carrer, Víctor
Barba, Clara
Martí, Meritxell
Coderch Negra, M. Luisa
author Alonso, Cristina
author_facet Alonso, Cristina
Collini, Ilaria
Carrer, Víctor
Barba, Clara
Martí, Meritxell
Coderch Negra, M. Luisa
author_role author
author2 Collini, Ilaria
Carrer, Víctor
Barba, Clara
Martí, Meritxell
Coderch Negra, M. Luisa
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Barba, Clara [0000-0002-3084-2925]
Martí, Meritxell [0000-0001-9681-6466]
Consejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]
dc.subject.none.fl_str_mv Synthetic membranes
Lanolin
Franz cells
Permeation profile
topic Synthetic membranes
Lanolin
Franz cells
Permeation profile
description Skin-penetration studies play an essential role in the selection of drugs for dermal or transdermal application. In vivo experiments in humans are not always possible for ethical, practical, or economic reasons, especially in the first part of the drug development. It is necessary to develop alternative methods using accessible and reproducible surrogates for in vivo human skin. The in vitro methodologies using biological membranes (human and animal skin) are recognized and well accepted as an alternative but present high inter- and intra-individual variability. Therefore, the formation of synthetic membranes has been studied to obtain skin- mimicking models for permeation studies. The aim of this work is to create lanolin-based artificial membranes that can mimic the absorption through the skin of compounds applied topically. A series of synthetic membranes using two different types of lanolin (water-extracted (WE) and solvent-extracted (SE)) were prepared. Next, the in vitro release test of three drugs (diclofenac sodium, ibuprofen and lidocaine) was performed on artificial membranes and on porcine skin placed on Franz cells. The percentage of release, flux, permeability coefficient, lag time, area under the curve, maximal concentration and time were determined for each compound in the different types of membrane. The results showed that lanolin membranes presented a strong diminution of permeability compared to most artificial membranes, leading to a very similar permeability to that of skin. The SE and WE membranes showed a diminution of transepidermal water loss and permeability of compounds compared with membranes alone. The results from WE membranes were similar to those found for the skin. The lanolin membranes were not capable of perfectly mimicking permeation through the skin, but they did have the same rank order of drug penetration as the skin. It may be deduced from these tests that these systems provide more reliable results for compounds with low to medium lipophilicity. The results demonstrated that new lanolin-based artificial membranes have the potential to be exploited as screening models for determining the permeability of a compound destined to be topically delivered.
publishDate 2020
dc.date.none.fl_str_mv 2020
2020
2020
dc.type.none.fl_str_mv info:eu-repo/semantics/article
http://purl.org/coar/resource_type/c_6501
Postprint
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/10261/212237
url http://hdl.handle.net/10261/212237
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv https://doi.org/10.1016/j.colsurfb.2020.111024
Sí
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:DIGITAL.CSIC. Repositorio Institucional del CSIC
instname:Consejo Superior de Investigaciones Científicas (CSIC)
instname_str Consejo Superior de Investigaciones Científicas (CSIC)
reponame_str DIGITAL.CSIC. Repositorio Institucional del CSIC
collection DIGITAL.CSIC. Repositorio Institucional del CSIC
repository.name.fl_str_mv
repository.mail.fl_str_mv
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