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...
| Autores: | , , , , , , , |
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| 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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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 |
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openAccess |
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application/pdf |
| dc.publisher.none.fl_str_mv |
MDPI |
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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 |
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Universidad de Barcelona |
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Dipòsit Digital de la UB |
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Dipòsit Digital de la UB |
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