Publication
Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management
| dc.contributor.author | Nunes, Andreia | |
| dc.contributor.author | Marto, Joana | |
| dc.contributor.author | Gonçalves, Lídia | |
| dc.contributor.author | Simões, Sandra | |
| dc.contributor.author | Félix, Rita | |
| dc.contributor.author | Ascenso, Andreia | |
| dc.contributor.author | Lopes, Francisca | |
| dc.contributor.author | Ribeiro, Helena | |
| dc.date.accessioned | 2024-01-19T19:59:41Z | |
| dc.date.available | 2024-01-19T19:59:41Z | |
| dc.date.issued | 2020-04-14 | |
| dc.date.updated | 2023-02-27T18:35:58Z | |
| dc.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/). | pt_PT |
| dc.description.abstract | 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. | pt_PT |
| dc.description.sponsorship | 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. | pt_PT |
| dc.description.version | info:eu-repo/semantics/publishedVersion | pt_PT |
| dc.identifier.citation | 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 | pt_PT |
| dc.identifier.doi | 10.3390/pharmaceutics12040358 | pt_PT |
| dc.identifier.issn | 1999-4923 | |
| dc.identifier.slug | cv-prod-2118931 | |
| dc.identifier.uri | http://hdl.handle.net/10451/62001 | |
| dc.language.iso | eng | pt_PT |
| dc.peerreviewed | yes | pt_PT |
| dc.publisher | MDPI | pt_PT |
| dc.relation | Research Institute for Medicines | |
| dc.relation.publisherversion | https://www.mdpi.com/1999-4923/12/4/358 | pt_PT |
| dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | pt_PT |
| dc.subject | human neutrophil elastase inhibitors | pt_PT |
| dc.subject | emulsions | pt_PT |
| dc.subject | microemulsions | pt_PT |
| dc.subject | psoriasis | pt_PT |
| dc.subject | topical application | pt_PT |
| dc.title | Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management | pt_PT |
| dc.type | journal article | |
| dspace.entity.type | Publication | |
| oaire.awardTitle | Research Institute for Medicines | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FDTP%2F04138%2F2019/PT | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/Concurso para Financiamento de Projetos de Investigação Científica e Desenvolvimento Tecnológico em Todos os Domínios Científicos - 2017/PTDC%2FMEC-DER%2F30198%2F2017/PT | |
| oaire.citation.issue | 4 | pt_PT |
| oaire.citation.startPage | 358 | pt_PT |
| oaire.citation.title | Pharmaceutics | pt_PT |
| oaire.citation.volume | 12 | pt_PT |
| oaire.fundingStream | 6817 - DCRRNI ID | |
| oaire.fundingStream | Concurso para Financiamento de Projetos de Investigação Científica e Desenvolvimento Tecnológico em Todos os Domínios Científicos - 2017 | |
| person.familyName | Germano Nunes | |
| person.familyName | Marques Marto | |
| person.familyName | Diogo Gonçalves | |
| person.familyName | Simões | |
| person.familyName | ascenso | |
| person.familyName | Lopes | |
| person.familyName | Ribeiro | |
| person.givenName | Andreia Alexandra | |
| person.givenName | Joana | |
| person.givenName | Lídia Maria | |
| person.givenName | Sandra | |
| person.givenName | andreia | |
| person.givenName | Francisca | |
| person.givenName | Helena | |
| person.identifier | C-2614-2014 | |
| person.identifier | 1570599 | |
| person.identifier.ciencia-id | 341E-127F-B86D | |
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| person.identifier.orcid | 0000-0002-6133-9943 | |
| person.identifier.orcid | 0000-0001-5523-5622 | |
| person.identifier.orcid | 0000-0002-6799-2740 | |
| person.identifier.orcid | 0000-0002-5685-1790 | |
| person.identifier.orcid | 0000-0002-8727-0614 | |
| person.identifier.orcid | 0000-0002-5350-147X | |
| person.identifier.orcid | 0000-0002-2429-7991 | |
| person.identifier.rid | E-2944-2015 | |
| person.identifier.scopus-author-id | 8724939200 | |
| person.identifier.scopus-author-id | 35896704400 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| rcaap.cv.cienciaid | 7211-22BA-86AD | Lídia Maria Diogo Gonçalves | |
| rcaap.rights | openAccess | pt_PT |
| rcaap.type | article | pt_PT |
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