Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management

Detalhes bibliográficos
Autor(a) principal: Nunes, Andreia
Data de Publicação: 2020
Outros Autores: Marto, Joana, Gonçalves, Lídia, Simões, Sandra, Félix, Rita, Ascenso, Andreia, Lopes, Francisca, Ribeiro, Helena
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10451/62001
Resumo: © 2020 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 Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Managementhuman neutrophil elastase inhibitorsemulsionsmicroemulsionspsoriasistopical application© 2020 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/).Human neutrophil elastase (HNE) is a serine protease that degrades matrix proteins. An excess of HNE may trigger several pathological conditions, such as psoriasis. In this work, we aimed to synthesize, characterize and formulate new HNE inhibitors with a 4-oxo-β-lactam scaffold with less toxicity, as well as therapeutic index in a psoriasis context. HNE inhibitors with 4-oxo-β-lactam scaffolds were synthesized and characterized by NMR, FTIR, melting point, mass spectrometry and elemental analysis. In vitro cytotoxicity and serine protease assays were performed. The compound with the highest cell viability (AAN-16) was selected to be incorporated in an emulsion (AAN-16 E) and in a microemulsion (AAN-16 ME). Formulations were characterized in terms of organoleptic properties, pH, rheology, droplet size distribution, in vitro drug release and in vivo psoriatic activity. All compounds were successfully synthesized according to analytical methodology, with good yields. Both formulations presented suitable physicochemical properties. AAN-16 E presented the most promising therapeutic effects in a murine model of psoriasis. Overall, new HNE inhibitors were synthesized with high and selective activity and incorporated into topical emulsions with potential to treat psoriasis.This work was supported by Fundação para a Ciência e a Tecnologia, Portugal (UID/DTP/04138/2019 to iMedUlisboa and and PTDC/MEC-DER/30198/2017) and Labodidática, Equipamentos de Laboratório e Didácticos L.da.MDPIRepositório da Universidade de LisboaNunes, AndreiaMarto, JoanaGonçalves, LídiaSimões, SandraFélix, RitaAscenso, AndreiaLopes, FranciscaRibeiro, Helena2024-01-19T19:59:41Z2020-04-142023-02-27T18:35:58Z2020-04-14T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10451/62001engNunes A, Marto J, Gonçalves LM, Simões S, Félix R, Ascenso A, et al. Novel and modified neutrophil elastase inhibitor loaded in topical formulations for psoriasis management. Pharmaceutics [Internet]. 14 de abril de 2020;12(4):358. Disponível em: https://www.mdpi.com/1999-4923/12/4/3581999-4923cv-prod-211893110.3390/pharmaceutics12040358info: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:RCAAP2024-01-22T01:20:20Zoai:repositorio.ul.pt:10451/62001Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T01:56:16.080022Repositório 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 Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
title Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
spellingShingle Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
Nunes, Andreia
human neutrophil elastase inhibitors
emulsions
microemulsions
psoriasis
topical application
title_short Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
title_full Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
title_fullStr Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
title_full_unstemmed Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
title_sort Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
author Nunes, Andreia
author_facet Nunes, Andreia
Marto, Joana
Gonçalves, Lídia
Simões, Sandra
Félix, Rita
Ascenso, Andreia
Lopes, Francisca
Ribeiro, Helena
author_role author
author2 Marto, Joana
Gonçalves, Lídia
Simões, Sandra
Félix, Rita
Ascenso, Andreia
Lopes, Francisca
Ribeiro, Helena
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Repositório da Universidade de Lisboa
dc.contributor.author.fl_str_mv Nunes, Andreia
Marto, Joana
Gonçalves, Lídia
Simões, Sandra
Félix, Rita
Ascenso, Andreia
Lopes, Francisca
Ribeiro, Helena
dc.subject.por.fl_str_mv human neutrophil elastase inhibitors
emulsions
microemulsions
psoriasis
topical application
topic human neutrophil elastase inhibitors
emulsions
microemulsions
psoriasis
topical application
description © 2020 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 2020
dc.date.none.fl_str_mv 2020-04-14
2020-04-14T00:00:00Z
2023-02-27T18:35:58Z
2024-01-19T19:59:41Z
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/10451/62001
url http://hdl.handle.net/10451/62001
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Nunes A, Marto J, Gonçalves LM, Simões S, Félix R, Ascenso A, et al. Novel and modified neutrophil elastase inhibitor loaded in topical formulations for psoriasis management. Pharmaceutics [Internet]. 14 de abril de 2020;12(4):358. Disponível em: https://www.mdpi.com/1999-4923/12/4/358
1999-4923
cv-prod-2118931
10.3390/pharmaceutics12040358
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
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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
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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
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