Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties

Detalhes bibliográficos
Autor(a) principal: Martins,P. S.
Data de Publicação: 2009
Outros Autores: Ribeiro,R. R., Bahia,A. P. C, M. Neto,R. L., Frézard,F., Pimenta,A. M. C., Melo,A. L., Le Moyec,L., Demicheli,C.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Brazilian Journal of Physics
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-97332009000200016
Resumo: β-cyclodextrin (β-CD) is widely used as a component of pharmaceutical formulations, classically to improve the solubility and oral bioavailability of poorly water-soluble drugs through formation of drug/β-CD inclusion complexes. Unexpectedly, the association of the highly water-soluble drug meglumine antimoniate (MA) with β-CD turned this antimonial compound orally-active in a murine model of leishmaniasis. To get insight into the mechanisms responsible for the enhanced oral efficacy of MA, the MA/β-CD composition was characterized physicochemically, using thermogravimetry, circular dichroism, mass spectrometry (ESI-MS), osmometry and photon correlation spectroscopy. The freeze-dried MA/β-CD was found to form nanoassemblies in water, as a result of multiple non-inclusion interactions between MA and β-CD, which behave as a sustained release system of the MA drug.
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spelling Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release propertiescyclodextrinantimonymeglumine antimoniatesustained releasenanobiotechnologyβ-cyclodextrin (β-CD) is widely used as a component of pharmaceutical formulations, classically to improve the solubility and oral bioavailability of poorly water-soluble drugs through formation of drug/β-CD inclusion complexes. Unexpectedly, the association of the highly water-soluble drug meglumine antimoniate (MA) with β-CD turned this antimonial compound orally-active in a murine model of leishmaniasis. To get insight into the mechanisms responsible for the enhanced oral efficacy of MA, the MA/β-CD composition was characterized physicochemically, using thermogravimetry, circular dichroism, mass spectrometry (ESI-MS), osmometry and photon correlation spectroscopy. The freeze-dried MA/β-CD was found to form nanoassemblies in water, as a result of multiple non-inclusion interactions between MA and β-CD, which behave as a sustained release system of the MA drug.Sociedade Brasileira de Física2009-04-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-97332009000200016Brazilian Journal of Physics v.39 n.1a 2009reponame:Brazilian Journal of Physicsinstname:Sociedade Brasileira de Física (SBF)instacron:SBF10.1590/S0103-97332009000200016info:eu-repo/semantics/openAccessMartins,P. S.Ribeiro,R. R.Bahia,A. P. CM. Neto,R. L.Frézard,F.Pimenta,A. M. C.Melo,A. L.Le Moyec,L.Demicheli,C.eng2009-07-03T00:00:00Zoai:scielo:S0103-97332009000200016Revistahttp://www.sbfisica.org.br/v1/home/index.php/pt/ONGhttps://old.scielo.br/oai/scielo-oai.phpsbfisica@sbfisica.org.br||sbfisica@sbfisica.org.br1678-44480103-9733opendoar:2009-07-03T00:00Brazilian Journal of Physics - Sociedade Brasileira de Física (SBF)false
dc.title.none.fl_str_mv Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties
title Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties
spellingShingle Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties
Martins,P. S.
cyclodextrin
antimony
meglumine antimoniate
sustained release
nanobiotechnology
title_short Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties
title_full Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties
title_fullStr Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties
title_full_unstemmed Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties
title_sort Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties
author Martins,P. S.
author_facet Martins,P. S.
Ribeiro,R. R.
Bahia,A. P. C
M. Neto,R. L.
Frézard,F.
Pimenta,A. M. C.
Melo,A. L.
Le Moyec,L.
Demicheli,C.
author_role author
author2 Ribeiro,R. R.
Bahia,A. P. C
M. Neto,R. L.
Frézard,F.
Pimenta,A. M. C.
Melo,A. L.
Le Moyec,L.
Demicheli,C.
author2_role author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Martins,P. S.
Ribeiro,R. R.
Bahia,A. P. C
M. Neto,R. L.
Frézard,F.
Pimenta,A. M. C.
Melo,A. L.
Le Moyec,L.
Demicheli,C.
dc.subject.por.fl_str_mv cyclodextrin
antimony
meglumine antimoniate
sustained release
nanobiotechnology
topic cyclodextrin
antimony
meglumine antimoniate
sustained release
nanobiotechnology
description β-cyclodextrin (β-CD) is widely used as a component of pharmaceutical formulations, classically to improve the solubility and oral bioavailability of poorly water-soluble drugs through formation of drug/β-CD inclusion complexes. Unexpectedly, the association of the highly water-soluble drug meglumine antimoniate (MA) with β-CD turned this antimonial compound orally-active in a murine model of leishmaniasis. To get insight into the mechanisms responsible for the enhanced oral efficacy of MA, the MA/β-CD composition was characterized physicochemically, using thermogravimetry, circular dichroism, mass spectrometry (ESI-MS), osmometry and photon correlation spectroscopy. The freeze-dried MA/β-CD was found to form nanoassemblies in water, as a result of multiple non-inclusion interactions between MA and β-CD, which behave as a sustained release system of the MA drug.
publishDate 2009
dc.date.none.fl_str_mv 2009-04-01
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=S0103-97332009000200016
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-97332009000200016
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/S0103-97332009000200016
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 Física
publisher.none.fl_str_mv Sociedade Brasileira de Física
dc.source.none.fl_str_mv Brazilian Journal of Physics v.39 n.1a 2009
reponame:Brazilian Journal of Physics
instname:Sociedade Brasileira de Física (SBF)
instacron:SBF
instname_str Sociedade Brasileira de Física (SBF)
instacron_str SBF
institution SBF
reponame_str Brazilian Journal of Physics
collection Brazilian Journal of Physics
repository.name.fl_str_mv Brazilian Journal of Physics - Sociedade Brasileira de Física (SBF)
repository.mail.fl_str_mv sbfisica@sbfisica.org.br||sbfisica@sbfisica.org.br
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