Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies

Detalhes bibliográficos
Autor(a) principal: Stecanella,Luciano Aparecido
Data de Publicação: 2013
Outros Autores: Taveira,Stephânia Fleury, Marreto,Ricardo Neves, Valadares,Marize C., Vieira,Marcelo de Sousa, Kato,Massuo Jorge, Lima,Eliana Martins
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Revista Brasileira de Farmacognosia (Online)
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2013000100021
Resumo: The most studied phyto constituent isolated from Virola surinamensis (Rol. ex Rottb.) Warb., Myristicaceae, is the tetrahydrofuran neolignan grandisin, which exhibits a series of biological activities, including trypanocidal, larvicidal and antitumoral. Due to its extremely low solubility, additional studies, including in vivo investigations are challenged by the difficulties in the development of an effective drug delivery system for grandisin. The encapsulation in polymeric nanoparticles is a very attractive alternative for overcoming some of these limitations. In this work, PLGA nanocapsules loaded with grandisin were developed in an attempt to optimize the efficacy of grandisin as an antitumoral drug, with high drug loading and efficiency, prolonged drug release and increased physical-chemical stability. Mean diameter of the nanocapsules was lower than 200 nm, with very low polydispersity. Encapsulation efficiency was above 90%. A sustained in vitro drug release was achieved for up to twenty days and cytotoxicity was markedly increased (IC50 for grandisin-NC and grandisin were 0.005 µM and 0.078 µM, respectively), indicating that polymeric nanocapsules are a potential drug delivery system for grandisin allowing the preparation of formulations viable for further in vivo studies.
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spelling Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studiescytotoxicitygrandisinPLGA nanocapsulessustained releaseThe most studied phyto constituent isolated from Virola surinamensis (Rol. ex Rottb.) Warb., Myristicaceae, is the tetrahydrofuran neolignan grandisin, which exhibits a series of biological activities, including trypanocidal, larvicidal and antitumoral. Due to its extremely low solubility, additional studies, including in vivo investigations are challenged by the difficulties in the development of an effective drug delivery system for grandisin. The encapsulation in polymeric nanoparticles is a very attractive alternative for overcoming some of these limitations. In this work, PLGA nanocapsules loaded with grandisin were developed in an attempt to optimize the efficacy of grandisin as an antitumoral drug, with high drug loading and efficiency, prolonged drug release and increased physical-chemical stability. Mean diameter of the nanocapsules was lower than 200 nm, with very low polydispersity. Encapsulation efficiency was above 90%. A sustained in vitro drug release was achieved for up to twenty days and cytotoxicity was markedly increased (IC50 for grandisin-NC and grandisin were 0.005 µM and 0.078 µM, respectively), indicating that polymeric nanocapsules are a potential drug delivery system for grandisin allowing the preparation of formulations viable for further in vivo studies.Sociedade Brasileira de Farmacognosia2013-02-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2013000100021Revista Brasileira de Farmacognosia v.23 n.1 2013reponame:Revista Brasileira de Farmacognosia (Online)instname:Sociedade Brasileira de Farmacognosia (SBFgnosia)instacron:SBFGNOSIA10.1590/S0102-695X2012005000128info:eu-repo/semantics/openAccessStecanella,Luciano AparecidoTaveira,Stephânia FleuryMarreto,Ricardo NevesValadares,Marize C.Vieira,Marcelo de SousaKato,Massuo JorgeLima,Eliana Martinseng2013-03-28T00:00:00Zoai:scielo:S0102-695X2013000100021Revistahttp://www.sbfgnosia.org.br/revista/https://old.scielo.br/oai/scielo-oai.phprbgnosia@ltf.ufpb.br1981-528X0102-695Xopendoar:2013-03-28T00:00Revista Brasileira de Farmacognosia (Online) - Sociedade Brasileira de Farmacognosia (SBFgnosia)false
dc.title.none.fl_str_mv Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
title Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
spellingShingle Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
Stecanella,Luciano Aparecido
cytotoxicity
grandisin
PLGA nanocapsules
sustained release
title_short Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
title_full Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
title_fullStr Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
title_full_unstemmed Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
title_sort Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
author Stecanella,Luciano Aparecido
author_facet Stecanella,Luciano Aparecido
Taveira,Stephânia Fleury
Marreto,Ricardo Neves
Valadares,Marize C.
Vieira,Marcelo de Sousa
Kato,Massuo Jorge
Lima,Eliana Martins
author_role author
author2 Taveira,Stephânia Fleury
Marreto,Ricardo Neves
Valadares,Marize C.
Vieira,Marcelo de Sousa
Kato,Massuo Jorge
Lima,Eliana Martins
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Stecanella,Luciano Aparecido
Taveira,Stephânia Fleury
Marreto,Ricardo Neves
Valadares,Marize C.
Vieira,Marcelo de Sousa
Kato,Massuo Jorge
Lima,Eliana Martins
dc.subject.por.fl_str_mv cytotoxicity
grandisin
PLGA nanocapsules
sustained release
topic cytotoxicity
grandisin
PLGA nanocapsules
sustained release
description The most studied phyto constituent isolated from Virola surinamensis (Rol. ex Rottb.) Warb., Myristicaceae, is the tetrahydrofuran neolignan grandisin, which exhibits a series of biological activities, including trypanocidal, larvicidal and antitumoral. Due to its extremely low solubility, additional studies, including in vivo investigations are challenged by the difficulties in the development of an effective drug delivery system for grandisin. The encapsulation in polymeric nanoparticles is a very attractive alternative for overcoming some of these limitations. In this work, PLGA nanocapsules loaded with grandisin were developed in an attempt to optimize the efficacy of grandisin as an antitumoral drug, with high drug loading and efficiency, prolonged drug release and increased physical-chemical stability. Mean diameter of the nanocapsules was lower than 200 nm, with very low polydispersity. Encapsulation efficiency was above 90%. A sustained in vitro drug release was achieved for up to twenty days and cytotoxicity was markedly increased (IC50 for grandisin-NC and grandisin were 0.005 µM and 0.078 µM, respectively), indicating that polymeric nanocapsules are a potential drug delivery system for grandisin allowing the preparation of formulations viable for further in vivo studies.
publishDate 2013
dc.date.none.fl_str_mv 2013-02-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2013000100021
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2013000100021
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/S0102-695X2012005000128
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv text/html
dc.publisher.none.fl_str_mv Sociedade Brasileira de Farmacognosia
publisher.none.fl_str_mv Sociedade Brasileira de Farmacognosia
dc.source.none.fl_str_mv Revista Brasileira de Farmacognosia v.23 n.1 2013
reponame:Revista Brasileira de Farmacognosia (Online)
instname:Sociedade Brasileira de Farmacognosia (SBFgnosia)
instacron:SBFGNOSIA
instname_str Sociedade Brasileira de Farmacognosia (SBFgnosia)
instacron_str SBFGNOSIA
institution SBFGNOSIA
reponame_str Revista Brasileira de Farmacognosia (Online)
collection Revista Brasileira de Farmacognosia (Online)
repository.name.fl_str_mv Revista Brasileira de Farmacognosia (Online) - Sociedade Brasileira de Farmacognosia (SBFgnosia)
repository.mail.fl_str_mv rbgnosia@ltf.ufpb.br
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