Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders

Abstract: Pranoprofen (PF)-loaded nanostructured lipid carriers (NLCs), prepared using a high-pressure homogenization method, have been optimized and characterized to improve the biopharmaceutical profile of the drug. The optimized PF-NLCs exhibited physicochemical characteristics and morphological...

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Autores: Rincón, María, Calpena Campmany, Ana Cristina, Fábrega Fernández, María José, Garduño Ramírez, María Luisa del Carmen, Espina García, Marta, Rodríguez Lagunas, María José, García López, María Luisa, Abrego Escobar, Guadalupe
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2018
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/132878
Acceso en línea:https://hdl.handle.net/2445/132878
Access Level:acceso abierto
Palabra clave:Agents antiinflamatoris
Nanopartícules
Malalties de la pell
Administració de medicaments
Antiinflammatory agents
Nanoparticles
Skin diseases
Administration of drugs
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spelling Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory DisordersRincón, MaríaCalpena Campmany, Ana CristinaFábrega Fernández, María JoséGarduño Ramírez, María Luisa del CarmenEspina García, MartaRodríguez Lagunas, María JoséGarcía López, María LuisaAbrego Escobar, GuadalupeAgents antiinflamatorisNanopartículesMalalties de la pellAdministració de medicamentsAntiinflammatory agentsNanoparticlesSkin diseasesAdministration of drugsAbstract: Pranoprofen (PF)-loaded nanostructured lipid carriers (NLCs), prepared using a high-pressure homogenization method, have been optimized and characterized to improve the biopharmaceutical profile of the drug. The optimized PF-NLCs exhibited physicochemical characteristics and morphological properties that were suitable for dermal application. Stability assays revealed good physical stability, and the release behavior of PF from these NLCs showed a sustained release pattern. Cell viability results revealed no toxicity. Ex vivo human skin permeation studies in Franz diffusion cells were performed to determine the influence of different skin penetration enhancers (pyrrolidone, decanol, octanoic acid, nonane, menthone, squalene, linoleic acid, and cineol) on skin penetration and retention of PF, being the highest dermal retention in the presence of linoleic acid. The selected formulations of NLCs exhibited a high retained amount of PF in the skin and no systemic effects. In vivo mice anti-inflammatory efficacy studies showed a significant reduction in dermal oedema. NLCs containing linoleic acid presented better anti-inflammatory efficacy by decreasing the production of interleukins in keratinocytes and monocytes. The biomechanical properties of skin revealed an occlusive effect and no hydration power. No signs of skin irritancy in vivo were detected. According to these results, dermal PF-NLCs could be an effective system for the delivery and controlled release of PF, improving its dermal retention, with reduced dermal oedema as a possible effect of this drug KEYWORDS: anti-inflammatory activity; linoleic acid; nanostructured lipid carriers; penetration enhancers; pranoprofen; skin deliveryMDPI2018info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://hdl.handle.net/2445/132878Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésReproducció del document publicat a: https://doi.org/10.3390/nano8121022Nanomaterials, 2018, vol. 8, num. 12, p. 1022-1050https://doi.org/10.3390/nano8121022cc-by (c) Rincón, María et al., 2018http://creativecommons.org/licenses/by/3.0/esinfo:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/1328782026-05-27T06:46:51Z
dc.title.none.fl_str_mv Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
title Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
spellingShingle Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
Rincón, María
Agents antiinflamatoris
Nanopartícules
Malalties de la pell
Administració de medicaments
Antiinflammatory agents
Nanoparticles
Skin diseases
Administration of drugs
title_short Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
title_full Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
title_fullStr Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
title_full_unstemmed Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
title_sort Development of Pranoprofen Loaded Nanostructured Lipid Carriers to Improve Its Release and Therapeutic Efficacy in Skin Inflammatory Disorders
dc.creator.none.fl_str_mv Rincón, María
Calpena Campmany, Ana Cristina
Fábrega Fernández, María José
Garduño Ramírez, María Luisa del Carmen
Espina García, Marta
Rodríguez Lagunas, María José
García López, María Luisa
Abrego Escobar, Guadalupe
author Rincón, María
author_facet Rincón, María
Calpena Campmany, Ana Cristina
Fábrega Fernández, María José
Garduño Ramírez, María Luisa del Carmen
Espina García, Marta
Rodríguez Lagunas, María José
García López, María Luisa
Abrego Escobar, Guadalupe
author_role author
author2 Calpena Campmany, Ana Cristina
Fábrega Fernández, María José
Garduño Ramírez, María Luisa del Carmen
Espina García, Marta
Rodríguez Lagunas, María José
García López, María Luisa
Abrego Escobar, Guadalupe
author2_role author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Agents antiinflamatoris
Nanopartícules
Malalties de la pell
Administració de medicaments
Antiinflammatory agents
Nanoparticles
Skin diseases
Administration of drugs
topic Agents antiinflamatoris
Nanopartícules
Malalties de la pell
Administració de medicaments
Antiinflammatory agents
Nanoparticles
Skin diseases
Administration of drugs
description Abstract: Pranoprofen (PF)-loaded nanostructured lipid carriers (NLCs), prepared using a high-pressure homogenization method, have been optimized and characterized to improve the biopharmaceutical profile of the drug. The optimized PF-NLCs exhibited physicochemical characteristics and morphological properties that were suitable for dermal application. Stability assays revealed good physical stability, and the release behavior of PF from these NLCs showed a sustained release pattern. Cell viability results revealed no toxicity. Ex vivo human skin permeation studies in Franz diffusion cells were performed to determine the influence of different skin penetration enhancers (pyrrolidone, decanol, octanoic acid, nonane, menthone, squalene, linoleic acid, and cineol) on skin penetration and retention of PF, being the highest dermal retention in the presence of linoleic acid. The selected formulations of NLCs exhibited a high retained amount of PF in the skin and no systemic effects. In vivo mice anti-inflammatory efficacy studies showed a significant reduction in dermal oedema. NLCs containing linoleic acid presented better anti-inflammatory efficacy by decreasing the production of interleukins in keratinocytes and monocytes. The biomechanical properties of skin revealed an occlusive effect and no hydration power. No signs of skin irritancy in vivo were detected. According to these results, dermal PF-NLCs could be an effective system for the delivery and controlled release of PF, improving its dermal retention, with reduced dermal oedema as a possible effect of this drug KEYWORDS: anti-inflammatory activity; linoleic acid; nanostructured lipid carriers; penetration enhancers; pranoprofen; skin delivery
publishDate 2018
dc.date.none.fl_str_mv 2018
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/132878
url https://hdl.handle.net/2445/132878
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Reproducció del document publicat a: https://doi.org/10.3390/nano8121022
Nanomaterials, 2018, vol. 8, num. 12, p. 1022-1050
https://doi.org/10.3390/nano8121022
dc.rights.none.fl_str_mv cc-by (c) Rincón, María et al., 2018
http://creativecommons.org/licenses/by/3.0/es
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by (c) Rincón, María et al., 2018
http://creativecommons.org/licenses/by/3.0/es
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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