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

2021Artigo científico Acesso aberto
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dc.contributor.authorMancini, Giuliana
dc.contributor.authorGonçalves, Lídia
dc.contributor.authorMarto, Joana
dc.contributor.authorCarvalho, Filomena Almeida
dc.contributor.authorSimões, Sandra
dc.contributor.authorRibeiro, Helena
dc.contributor.authorAlmeida, António José
dc.date.accessioned2022-09-07T10:39:46Z
dc.date.available2022-09-07T10:39:46Z
dc.date.issued2021
dc.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/).pt_PT
dc.description.abstractInnovative 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.pt_PT
dc.description.sponsorshipThis 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.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationPharmaceutics. 2021 Mar 3;13(3):328pt_PT
dc.identifier.doi10.3390/pharmaceutics13030328pt_PT
dc.identifier.eissn1999-4923
dc.identifier.urihttp://hdl.handle.net/10451/54340
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relationSFRH/BDE/3379/5/2009pt_PT
dc.relationResearch Institute for Medicines
dc.relationResearch Institute for Medicines
dc.relationNot Available
dc.relationNot Available
dc.relation.publisherversionhttps://www.mdpi.com/journal/pharmaceuticspt_PT
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectAnti-inflammatory activitypt_PT
dc.subjectDermal deliverypt_PT
dc.subjectEtofenamatept_PT
dc.subjectHydrogelspt_PT
dc.subjectIbuprofenpt_PT
dc.subjectSolid Lipid Nanoparticles (SLN)pt_PT
dc.titleIncreased therapeutic efficacy of SLN containing Etofenamate and Ibuprofen in topical treatment of inflammationpt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardNumberUID/DTP/04138/2019
oaire.awardNumberUIDB/04138/2020
oaire.awardNumberCEECIND/03143/2017/CP1476/CT0005
oaire.awardNumberCEECINST/00145/2018/CP1571/CT0001
oaire.awardTitleResearch Institute for Medicines
oaire.awardTitleResearch Institute for Medicines
oaire.awardTitleNot Available
oaire.awardTitleNot Available
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FDTP%2F04138%2F2019/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F04138%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/CEEC IND 2017/CEECIND%2F03143%2F2017%2FCP1476%2FCT0005/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/CEEC INST 2018/CEECINST%2F00145%2F2018%2FCP1571%2FCT0001/PT
oaire.citation.issue3pt_PT
oaire.citation.titlePharmaceuticspt_PT
oaire.citation.volume13pt_PT
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStreamCEEC IND 2017
oaire.fundingStreamCEEC INST 2018
person.familyNameDiogo Gonçalves
person.familyNameMarques Marto
person.familyNameCarvalho
person.familyNameSimões
person.familyNameRibeiro
person.familyNameLeitão das Neves Almeida
person.givenNameLídia Maria
person.givenNameJoana
person.givenNameFilomena
person.givenNameSandra
person.givenNameHelena
person.givenNameAntónio José
person.identifierC-2614-2014
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person.identifier.ciencia-id4011-196E-E4EA
person.identifier.ciencia-id161F-B79B-D660
person.identifier.ciencia-id8312-F853-C47A
person.identifier.orcid0000-0002-6799-2740
person.identifier.orcid0000-0001-5523-5622
person.identifier.orcid0000-0001-6088-3894
person.identifier.orcid0000-0002-5685-1790
person.identifier.orcid0000-0002-2429-7991
person.identifier.orcid0000-0002-7807-4726
person.identifier.ridM-9202-2013
person.identifier.ridE-2944-2015
person.identifier.scopus-author-id7103069694
person.identifier.scopus-author-id8724939200
person.identifier.scopus-author-id35896704400
person.identifier.scopus-author-id57195052432
project.funder.identifierhttp://doi.org/10.13039/501100001871
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project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
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IMM - Artigos em Revistas Internacionais
FF - CiênciaVitae - Faculdade de Farmácia
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