Increased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammation
Autor(a) principal: | |
---|---|
Data de Publicação: | 2021 |
Outros Autores: | , , , , , |
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/). |
id |
RCAP_fbb67e4146be6bc8655d7688e4d9ee0c |
---|---|
oai_identifier_str |
oai:repositorio.ul.pt:10451/54340 |
network_acronym_str |
RCAP |
network_name_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository_id_str |
7160 |
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 |
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 |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
instname_str |
Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
instacron_str |
RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository.name.fl_str_mv |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
repository.mail.fl_str_mv |
|
_version_ |
1799134599507345408 |