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Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum

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Resumo:Quercetin and biapigenin are antioxidant and neuroprotective compounds present in Hypericum perforatum, with potential application in neurodegenerative diseases. Quercetin has shown to have excellent antioxidant activities. Biapigenin possesses a distinctive mechanism of action, preventing the onset of calcium deregulation and mitochondrial dysfunction. The main aim of this study was to establish a new delivery system encapsulating H. perforatum neuroprotective fraction, isolated from it,containing quercetin and biapigenin into poly(Ɛ-caprolactone) (PCL) nanoparticles. It also aimed to study its hepatoprotective potential. Different formulation parameters were optimized, resulting in a stable formulation of polymer:compounds ratio 1:0.1 with a mean particle size of 185nm, zeta potential around -20mV and association efficiency close to 100%. Compounds in vitro release, under physiological conditions, showed an initial burst followed by a sustained release. The antioxidant functional properties of these compounds were not altered by encapsulation. PCL-loaded nanoparticles protected HepG2 cells from intrinsic compound toxicity at high concentrations. Depending on the incubation regimen, quercetin-biapigenin PCL-loaded nanoparticles or free compounds were more effective in protecting HepG2 cells against tert-butylhydroperoxide-induced toxicity. This is the first report of the encapsulation of a quercetin-biapigenin mixture in a polymeric matrix, specifically, in PCL, with synergic anti-oxidant and hepatoprotective effects.
Autores principais:Oliveira, Ana Isabel
Outros Autores:Pinho, Cláudia; Fonte, Pedro; Sarmento, Bruno; Dias, Alberto Carlos Pires
Assunto:Hep G2 Cells Humans Hypericum perforatum Antioxidants Drug Carriers Nanoparticles Neuroprotective Agents Polyesters Quercetin Biapigenin Hepatoprotective In vitro release Anti-oxidant Anti-oxidant
Ano:2018
País:Portugal
Tipo de documento:artigo
Tipo de acesso:acesso aberto
Instituição associada:Universidade do Minho
Idioma:inglês
Origem:RepositóriUM - Universidade do Minho
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author Oliveira, Ana Isabel
author2 Pinho, Cláudia
Fonte, Pedro
Sarmento, Bruno
Dias, Alberto Carlos Pires
author2_role author
author
author
author
author_facet Oliveira, Ana Isabel
Pinho, Cláudia
Fonte, Pedro
Sarmento, Bruno
Dias, Alberto Carlos Pires
author_role author
contributor_name_str_mv Universidade do Minho
country_str PT
creators_json_txt [{\"Person.name\":\"Oliveira, Ana Isabel\"},{\"Person.name\":\"Pinho, Cláudia\"},{\"Person.name\":\"Fonte, Pedro\"},{\"Person.name\":\"Sarmento, Bruno\"},{\"Person.name\":\"Dias, Alberto Carlos Pires\"}]
datacite.contributors.contributor.contributorName.fl_str_mv Universidade do Minho
datacite.creators.creator.creatorName.fl_str_mv Oliveira, Ana Isabel
Pinho, Cláudia
Fonte, Pedro
Sarmento, Bruno
Dias, Alberto Carlos Pires
datacite.date.Accepted.fl_str_mv 2018-01-01T00:00:00Z
datacite.date.available.fl_str_mv 2021-06-16T09:47:54Z
datacite.date.embargoed.fl_str_mv 2021-06-16T09:47:54Z
datacite.rights.fl_str_mv http://purl.org/coar/access_right/c_abf2
datacite.subjects.subject.fl_str_mv Hep G2 Cells
Humans
Hypericum perforatum
Antioxidants
Drug Carriers
Nanoparticles
Neuroprotective Agents
Polyesters
Quercetin
Biapigenin
Hepatoprotective
In vitro release
Anti-oxidant
Anti-oxidant
datacite.titles.title.fl_str_mv Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
dc.contributor.none.fl_str_mv Universidade do Minho
dc.creator.none.fl_str_mv Oliveira, Ana Isabel
Pinho, Cláudia
Fonte, Pedro
Sarmento, Bruno
Dias, Alberto Carlos Pires
dc.date.Accepted.fl_str_mv 2018-01-01T00:00:00Z
dc.date.available.fl_str_mv 2021-06-16T09:47:54Z
dc.date.embargoed.fl_str_mv 2021-06-16T09:47:54Z
dc.format.none.fl_str_mv application/pdf
dc.identifier.none.fl_str_mv https://hdl.handle.net/1822/73411
dc.language.none.fl_str_mv eng
dc.publisher.none.fl_str_mv Elsevier
dc.rights.none.fl_str_mv http://purl.org/coar/access_right/c_abf2
dc.subject.none.fl_str_mv Hep G2 Cells
Humans
Hypericum perforatum
Antioxidants
Drug Carriers
Nanoparticles
Neuroprotective Agents
Polyesters
Quercetin
Biapigenin
Hepatoprotective
In vitro release
Anti-oxidant
Anti-oxidant
dc.title.fl_str_mv Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
dc.type.none.fl_str_mv http://purl.org/coar/resource_type/c_6501
description Quercetin and biapigenin are antioxidant and neuroprotective compounds present in Hypericum perforatum, with potential application in neurodegenerative diseases. Quercetin has shown to have excellent antioxidant activities. Biapigenin possesses a distinctive mechanism of action, preventing the onset of calcium deregulation and mitochondrial dysfunction. The main aim of this study was to establish a new delivery system encapsulating H. perforatum neuroprotective fraction, isolated from it,containing quercetin and biapigenin into poly(Ɛ-caprolactone) (PCL) nanoparticles. It also aimed to study its hepatoprotective potential. Different formulation parameters were optimized, resulting in a stable formulation of polymer:compounds ratio 1:0.1 with a mean particle size of 185nm, zeta potential around -20mV and association efficiency close to 100%. Compounds in vitro release, under physiological conditions, showed an initial burst followed by a sustained release. The antioxidant functional properties of these compounds were not altered by encapsulation. PCL-loaded nanoparticles protected HepG2 cells from intrinsic compound toxicity at high concentrations. Depending on the incubation regimen, quercetin-biapigenin PCL-loaded nanoparticles or free compounds were more effective in protecting HepG2 cells against tert-butylhydroperoxide-induced toxicity. This is the first report of the encapsulation of a quercetin-biapigenin mixture in a polymeric matrix, specifically, in PCL, with synergic anti-oxidant and hepatoprotective effects.
dirty 0
eu_rights_str_mv openAccess
format article
fulltext.url.fl_str_mv https://prod-dspace.uminho.pt/bitstreams/b30aaeda-7781-4279-848d-f36f4f7b0de4/download
id rum_a3cdcbfb779fdec07e8c390751d87f64
identifier.url.fl_str_mv https://hdl.handle.net/1822/73411
instacron_str repositorium
institution Universidade do Minho
instname_str Universidade do Minho
language eng
network_acronym_str rum
network_name_str RepositóriUM - Universidade do Minho
oai_identifier_str oai:repositorium.uminho.pt:1822/73411
organization_str_mv urn:organizationAcronym:repositorium
person_str_mv Oliveira, Ana Isabel
Pinho, Cláudia
Fonte, Pedro
Sarmento, Bruno
Dias, Alberto Carlos Pires
publishDate 2018
publisher.none.fl_str_mv Elsevier
reponame_str RepositóriUM - Universidade do Minho
repository_id_str urn:repositoryAcronym:rum
service_str_mv urn:repositoryAcronym:rum
spelling engElsevierporQuercetin and biapigenin are antioxidant and neuroprotective compounds present in Hypericum perforatum, with potential application in neurodegenerative diseases. Quercetin has shown to have excellent antioxidant activities. Biapigenin possesses a distinctive mechanism of action, preventing the onset of calcium deregulation and mitochondrial dysfunction. The main aim of this study was to establish a new delivery system encapsulating H. perforatum neuroprotective fraction, isolated from it,containing quercetin and biapigenin into poly(Ɛ-caprolactone) (PCL) nanoparticles. It also aimed to study its hepatoprotective potential. Different formulation parameters were optimized, resulting in a stable formulation of polymer:compounds ratio 1:0.1 with a mean particle size of 185nm, zeta potential around -20mV and association efficiency close to 100%. Compounds in vitro release, under physiological conditions, showed an initial burst followed by a sustained release. The antioxidant functional properties of these compounds were not altered by encapsulation. PCL-loaded nanoparticles protected HepG2 cells from intrinsic compound toxicity at high concentrations. Depending on the incubation regimen, quercetin-biapigenin PCL-loaded nanoparticles or free compounds were more effective in protecting HepG2 cells against tert-butylhydroperoxide-induced toxicity. This is the first report of the encapsulation of a quercetin-biapigenin mixture in a polymeric matrix, specifically, in PCL, with synergic anti-oxidant and hepatoprotective effects.application/pdfporDevelopment, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatumOliveira, Ana IsabelPinho, CláudiaFonte, PedroSarmento, BrunoDias, Alberto Carlos PiresHostingInstitutionOrganizationalUniversidade do Minhoe-mailmailto:repositorium@usdb.uminho.ptrepositorium@usdb.uminho.ptISSNIsPartOf0141-8130DOIIsPartOf10.1016/j.ijbiomac.2017.10.1032021-06-16T09:47:54Z20182018-01-01T00:00:00ZHandlehttps://hdl.handle.net/1822/73411http://purl.org/coar/access_right/c_abf2open accessHep G2 CellsHumansHypericum perforatumAntioxidantsDrug CarriersNanoparticlesNeuroprotective AgentsPolyestersQuercetinBiapigeninHepatoprotectiveIn vitro releaseAnti-oxidantAnti-oxidant2301241 bytesliteraturehttp://purl.org/coar/resource_type/c_6501journal articlehttp://purl.org/coar/access_right/c_abf2application/pdffulltexthttps://prod-dspace.uminho.pt/bitstreams/b30aaeda-7781-4279-848d-f36f4f7b0de4/download
spellingShingle Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
Oliveira, Ana Isabel
Hep G2 Cells
Humans
Hypericum perforatum
Antioxidants
Drug Carriers
Nanoparticles
Neuroprotective Agents
Polyesters
Quercetin
Biapigenin
Hepatoprotective
In vitro release
Anti-oxidant
Anti-oxidant
status SINGLETON
subject.fl_str_mv Hep G2 Cells
Humans
Hypericum perforatum
Antioxidants
Drug Carriers
Nanoparticles
Neuroprotective Agents
Polyesters
Quercetin
Biapigenin
Hepatoprotective
In vitro release
Anti-oxidant
Anti-oxidant
title Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
title_full Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
title_fullStr Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
title_full_unstemmed Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
title_short Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
title_sort Development, characterization, antioxidant and hepatoprotective properties of poly(Ɛ-caprolactone) nanoparticles loaded with a neuroprotective fraction of Hypericum perforatum
topic Hep G2 Cells
Humans
Hypericum perforatum
Antioxidants
Drug Carriers
Nanoparticles
Neuroprotective Agents
Polyesters
Quercetin
Biapigenin
Hepatoprotective
In vitro release
Anti-oxidant
Anti-oxidant
topic_facet Hep G2 Cells
Humans
Hypericum perforatum
Antioxidants
Drug Carriers
Nanoparticles
Neuroprotective Agents
Polyesters
Quercetin
Biapigenin
Hepatoprotective
In vitro release
Anti-oxidant
Anti-oxidant
url https://hdl.handle.net/1822/73411
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