Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance

Detalhes bibliográficos
Autor(a) principal: Beck,Ruy C. R.
Data de Publicação: 2005
Outros Autores: Pohlmann,Adriana R., Benvenutti,Edilson V., Dalla Costa,Teresa, Guterres,Sílvia S.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Journal of the Brazilian Chemical Society (Online)
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532005000700022
Resumo: This work reports the preparation and characterization of polymeric nanostructure-coated diclofenac-loaded microparticles. After spray-drying, powders presented 80% of yield and encapsulation efficiency of 83%. SEM analyses showed nanostructures adsorbed onto the surface of microparticles presenting surface area (BET) and pore volumes (BJH) (83 m² g-1, 0.10 cm³ g-1) smaller than the uncoated-core (163 m² g-1, 0.25 cm³ g-1). In vitro drug release experiments at pH 5.0 and 7.4 showed dissolution efficiencies of 34% and 78% (uncoated-core), 74% and 83% (physical mixture of raw materials), and 58% and 85% (nanostructure-coated microparticles), respectively. Mathematical modeling of the dissolution profiles fitted a biexponential model at pH 5.0 and a monoexponential model at pH 7.4. Regarding the digestive tolerance experiments, the total lesional indexes were 156.1 ± 48.5 for sodium diclofenac aqueous solution, 132.4 ± 45.7 for uncoated-core, 109.1 ± 35.8 for physical mixture and 29.9 ± 12.1 for microparticles showing a protective effect of these microparticles against the mucosal diclofenac damage. This strategy of coating presents a potential use for oral administration of drugs.
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spelling Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerancediclofenacpolymernanostructure-coatingmicroparticlesgastrointestinal toleranceThis work reports the preparation and characterization of polymeric nanostructure-coated diclofenac-loaded microparticles. After spray-drying, powders presented 80% of yield and encapsulation efficiency of 83%. SEM analyses showed nanostructures adsorbed onto the surface of microparticles presenting surface area (BET) and pore volumes (BJH) (83 m² g-1, 0.10 cm³ g-1) smaller than the uncoated-core (163 m² g-1, 0.25 cm³ g-1). In vitro drug release experiments at pH 5.0 and 7.4 showed dissolution efficiencies of 34% and 78% (uncoated-core), 74% and 83% (physical mixture of raw materials), and 58% and 85% (nanostructure-coated microparticles), respectively. Mathematical modeling of the dissolution profiles fitted a biexponential model at pH 5.0 and a monoexponential model at pH 7.4. Regarding the digestive tolerance experiments, the total lesional indexes were 156.1 ± 48.5 for sodium diclofenac aqueous solution, 132.4 ± 45.7 for uncoated-core, 109.1 ± 35.8 for physical mixture and 29.9 ± 12.1 for microparticles showing a protective effect of these microparticles against the mucosal diclofenac damage. This strategy of coating presents a potential use for oral administration of drugs.Sociedade Brasileira de Química2005-12-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532005000700022Journal of the Brazilian Chemical Society v.16 n.6a 2005reponame:Journal of the Brazilian Chemical Society (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.1590/S0103-50532005000700022info:eu-repo/semantics/openAccessBeck,Ruy C. R.Pohlmann,Adriana R.Benvenutti,Edilson V.Dalla Costa,TeresaGuterres,Sílvia S.eng2006-01-04T00:00:00Zoai:scielo:S0103-50532005000700022Revistahttp://jbcs.sbq.org.brONGhttps://old.scielo.br/oai/scielo-oai.php||office@jbcs.sbq.org.br1678-47900103-5053opendoar:2006-01-04T00:00Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)false
dc.title.none.fl_str_mv Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
title Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
spellingShingle Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
Beck,Ruy C. R.
diclofenac
polymer
nanostructure-coating
microparticles
gastrointestinal tolerance
title_short Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
title_full Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
title_fullStr Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
title_full_unstemmed Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
title_sort Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
author Beck,Ruy C. R.
author_facet Beck,Ruy C. R.
Pohlmann,Adriana R.
Benvenutti,Edilson V.
Dalla Costa,Teresa
Guterres,Sílvia S.
author_role author
author2 Pohlmann,Adriana R.
Benvenutti,Edilson V.
Dalla Costa,Teresa
Guterres,Sílvia S.
author2_role author
author
author
author
dc.contributor.author.fl_str_mv Beck,Ruy C. R.
Pohlmann,Adriana R.
Benvenutti,Edilson V.
Dalla Costa,Teresa
Guterres,Sílvia S.
dc.subject.por.fl_str_mv diclofenac
polymer
nanostructure-coating
microparticles
gastrointestinal tolerance
topic diclofenac
polymer
nanostructure-coating
microparticles
gastrointestinal tolerance
description This work reports the preparation and characterization of polymeric nanostructure-coated diclofenac-loaded microparticles. After spray-drying, powders presented 80% of yield and encapsulation efficiency of 83%. SEM analyses showed nanostructures adsorbed onto the surface of microparticles presenting surface area (BET) and pore volumes (BJH) (83 m² g-1, 0.10 cm³ g-1) smaller than the uncoated-core (163 m² g-1, 0.25 cm³ g-1). In vitro drug release experiments at pH 5.0 and 7.4 showed dissolution efficiencies of 34% and 78% (uncoated-core), 74% and 83% (physical mixture of raw materials), and 58% and 85% (nanostructure-coated microparticles), respectively. Mathematical modeling of the dissolution profiles fitted a biexponential model at pH 5.0 and a monoexponential model at pH 7.4. Regarding the digestive tolerance experiments, the total lesional indexes were 156.1 ± 48.5 for sodium diclofenac aqueous solution, 132.4 ± 45.7 for uncoated-core, 109.1 ± 35.8 for physical mixture and 29.9 ± 12.1 for microparticles showing a protective effect of these microparticles against the mucosal diclofenac damage. This strategy of coating presents a potential use for oral administration of drugs.
publishDate 2005
dc.date.none.fl_str_mv 2005-12-01
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=S0103-50532005000700022
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532005000700022
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/S0103-50532005000700022
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 Química
publisher.none.fl_str_mv Sociedade Brasileira de Química
dc.source.none.fl_str_mv Journal of the Brazilian Chemical Society v.16 n.6a 2005
reponame:Journal of the Brazilian Chemical Society (Online)
instname:Sociedade Brasileira de Química (SBQ)
instacron:SBQ
instname_str Sociedade Brasileira de Química (SBQ)
instacron_str SBQ
institution SBQ
reponame_str Journal of the Brazilian Chemical Society (Online)
collection Journal of the Brazilian Chemical Society (Online)
repository.name.fl_str_mv Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)
repository.mail.fl_str_mv ||office@jbcs.sbq.org.br
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