Nanostructure-coated diclofenac-loaded microparticles: preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance
Autor(a) principal: | |
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Data de Publicação: | 2005 |
Outros Autores: | , , , |
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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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 |
_version_ |
1750318166624436224 |