Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation

Detalhes bibliográficos
Autor(a) principal: Mancini, Giuliana
Data de Publicação: 2021
Outros Autores: Gonçalves, Lídia, Marto, Joana, Carvalho, Filomena Almeida, Simões, Sandra, Ribeiro, Helena, Almeida, António José
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10451/54340
Resumo: © 2021 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
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spelling Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammationAnti-inflammatory activityDermal deliveryEtofenamateHydrogelsIbuprofenSolid Lipid Nanoparticles (SLN)© 2021 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).Innovative formulations, including solid lipid nanoparticles (SLNs), have been sought to improve skin permeation of non-steroidal anti-inflammatory drugs (NSAIDs). The present study explores the use of SLNs, prepared using a fusion-emulsification method, to increase skin permeation and in vivo activity of two relevant NSAIDs: A liquid molecule (etofenamate) and a solid one (ibuprofen), formulated in a 2% hydroxypropyl methylcellulose gel through the gelation of SLN suspensions. Compritol® 888 ATO and Tween® 80 were used as a solid lipid and a surfactant, respectively. All production steps were up scalable, resulting in SLNs with high encapsulation efficiency (>90%), a mean particle size of <250 nm, a polydispersity index <0.2, and that were stable for 12 months. In vitro permeation, using human skin in Franz diffusion cells, showed increased permeation and similar cell viability in Df and HaCaT cell lines for SLN formulations when compared to commercial formulations of etofenamate (Reumon® Gel 5%) and ibuprofen (Ozonol® 5%). In vivo activity in the rat paw edema inflammation model showed that SLN hydrogels containing lower doses of etofenamate (8.3 times lower) and ibuprofen (16.6 times lower) produced similar effects compared to the commercial formulations, while decreasing edema and inflammatory cell infiltration, and causing no histological changes in the epidermis. These studies demonstrate that encapsulation in SLNs associated to a suitable hydrogel is a promising technological approach to NSAIDs dermal application.This research was funded by the Portuguese Foundation for Science and Technology (FCT) through the grant SFRH/BDE/3379/5/2009, the programs UID/DTP/04138/2019, and UIDB/04138/2020. Authors acknowledge the generous donation of chemicals and technical support in the release/permeation assays from António Bica and Rui Rodrigues (LEF, Laboratórios de Estudos Farmacêuticos, Portugal). Principal Researcher grant CEECIND/03143/2017 (to L.M.D.G.) and Assistant Professor grant CEECINST/00145/2018 (to J.M.) are acknowledged.MDPIRepositório da Universidade de LisboaMancini, GiulianaGonçalves, LídiaMarto, JoanaCarvalho, Filomena AlmeidaSimões, SandraRibeiro, HelenaAlmeida, António José2022-09-07T10:39:46Z20212021-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10451/54340engPharmaceutics. 2021 Mar 3;13(3):32810.3390/pharmaceutics130303281999-4923info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-11-08T17:00:01Zoai:repositorio.ul.pt:10451/54340Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T22:04:48.506494Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
title Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
spellingShingle Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
Mancini, Giuliana
Anti-inflammatory activity
Dermal delivery
Etofenamate
Hydrogels
Ibuprofen
Solid Lipid Nanoparticles (SLN)
title_short Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
title_full Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
title_fullStr Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
title_full_unstemmed Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
title_sort Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
author Mancini, Giuliana
author_facet Mancini, Giuliana
Gonçalves, Lídia
Marto, Joana
Carvalho, Filomena Almeida
Simões, Sandra
Ribeiro, Helena
Almeida, António José
author_role author
author2 Gonçalves, Lídia
Marto, Joana
Carvalho, Filomena Almeida
Simões, Sandra
Ribeiro, Helena
Almeida, António José
author2_role author
author
author
author
author
author
dc.contributor.none.fl_str_mv Repositório da Universidade de Lisboa
dc.contributor.author.fl_str_mv Mancini, Giuliana
Gonçalves, Lídia
Marto, Joana
Carvalho, Filomena Almeida
Simões, Sandra
Ribeiro, Helena
Almeida, António José
dc.subject.por.fl_str_mv Anti-inflammatory activity
Dermal delivery
Etofenamate
Hydrogels
Ibuprofen
Solid Lipid Nanoparticles (SLN)
topic Anti-inflammatory activity
Dermal delivery
Etofenamate
Hydrogels
Ibuprofen
Solid Lipid Nanoparticles (SLN)
description © 2021 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
publishDate 2021
dc.date.none.fl_str_mv 2021
2021-01-01T00:00:00Z
2022-09-07T10:39:46Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10451/54340
url http://hdl.handle.net/10451/54340
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Pharmaceutics. 2021 Mar 3;13(3):328
10.3390/pharmaceutics13030328
1999-4923
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
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