Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
Autor(a) principal: | |
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Data de Publicação: | 2013 |
Outros Autores: | , , , , , |
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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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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1752122468255924224 |