A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads
Autor(a) principal: | |
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Data de Publicação: | 2013 |
Outros Autores: | , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/1822/36850 |
Resumo: | The aim of the research effort entertained herein was to develop, evaluate and fully characterize a multiparticulate floating gastroretentive system for the modified release of zidovudine (AZT), an antiretroviral drug. AZT was used as a water-soluble model drug at therapeutic doses. The floating gastroretentive system was obtained via polymer coating of calcium silicate-adsorbed AZT. The proposed system was evaluated in vitro for particle micromorphology, lag time for floating and duration of floating, drug loading capacity, drug release profile, and drug release kinetics. The physicochemical properties of AZT were evaluated by scanning electron microscopy (SEM) analyses, differential scanning calorimetry (DSC) analyses, X-ray diffraction (XRD) analyses, and infrared spectroscopy (FTIR) analyses. Results from SEM analysis of the AZT-containing floating gastroretentive granules allowed observation of an irregular surface and the apparent absence of pores. Floating of the AZT-containing gastroretentive granules was immediately achieved, that is lag time for floating was virtually zero and duration of floating was higher than 12 h. The drug loading capacity of the floating gastroretentive granules was ca. 81.09 ± 14.66%, and the release system thus obtained exhibited an extended drug release profile. Results from DSC and XRD analyses showed a modification in the AZT solid state, while the FTIR spectroscopy analyses revealed that the chemical structure of AZT remained unchanged upon adsorption to calcium silicate followed by polymeric coating. Hence, the coated granules produced presented gastroretentive, floating, and extended drug release properties. |
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A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads3 - azidothymidine (AZT)Cal-sil floating granulesGastroretentive floating systemExtended drug releaseZidovudine (AZT)Polymer coatingCiências Naturais::Ciências BiológicasCiências Médicas::Biotecnologia MédicaThe aim of the research effort entertained herein was to develop, evaluate and fully characterize a multiparticulate floating gastroretentive system for the modified release of zidovudine (AZT), an antiretroviral drug. AZT was used as a water-soluble model drug at therapeutic doses. The floating gastroretentive system was obtained via polymer coating of calcium silicate-adsorbed AZT. The proposed system was evaluated in vitro for particle micromorphology, lag time for floating and duration of floating, drug loading capacity, drug release profile, and drug release kinetics. The physicochemical properties of AZT were evaluated by scanning electron microscopy (SEM) analyses, differential scanning calorimetry (DSC) analyses, X-ray diffraction (XRD) analyses, and infrared spectroscopy (FTIR) analyses. Results from SEM analysis of the AZT-containing floating gastroretentive granules allowed observation of an irregular surface and the apparent absence of pores. Floating of the AZT-containing gastroretentive granules was immediately achieved, that is lag time for floating was virtually zero and duration of floating was higher than 12 h. The drug loading capacity of the floating gastroretentive granules was ca. 81.09 ± 14.66%, and the release system thus obtained exhibited an extended drug release profile. Results from DSC and XRD analyses showed a modification in the AZT solid state, while the FTIR spectroscopy analyses revealed that the chemical structure of AZT remained unchanged upon adsorption to calcium silicate followed by polymeric coating. Hence, the coated granules produced presented gastroretentive, floating, and extended drug release properties.Research Scientist fellowship ( FAPESP Ref. No. 2011/51077 - 8 ) is hereby gratefully acknowledged. The authors also wish to thank Nortec Química (Rio de Janeiro RJ, Brazil) for providing the reference materials, and Almapal (São Paulo SP, Brazil) and Cristalia Laboratories (Itapira SP, Brazil) for providing the samples. SAU - FAR: The Portuguese Science and Technology Foundation ( PTDC/SAU - FAR/113100/2009)Academic JournalsUniversidade do MinhoYoshida, Valquíria M. H.Granato, ElisGremião, Maria Palmira DaflonBalcão, V. M.Vila, Marta M. D. C.Oliveira Junior, José M.Severino, PatríciaSouto, Eliana B.Chaud, Marco V.2013-122013-12-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/1822/36850engYoshida, Valquíria M. H.; Granato, Elis; Gremião, Maria Palmira Daflon; Balcão, V. M.; Vila, Marta M. D. C.; Oliveira Junior, José M.; Severino, Patrícia; Souto, Eliana B.; Chaud, Marco V., A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads. African Journal of Pharmacy and Pharmacology, 7(46), 2937-2946, 20131996-081610.5897/AJPP2013.3808info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-07-21T12:42:10Zoai:repositorium.sdum.uminho.pt:1822/36850Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T19:39:20.816030Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads |
title |
A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads |
spellingShingle |
A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads Yoshida, Valquíria M. H. 3 - azidothymidine (AZT) Cal-sil floating granules Gastroretentive floating system Extended drug release Zidovudine (AZT) Polymer coating Ciências Naturais::Ciências Biológicas Ciências Médicas::Biotecnologia Médica |
title_short |
A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads |
title_full |
A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads |
title_fullStr |
A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads |
title_full_unstemmed |
A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads |
title_sort |
A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads |
author |
Yoshida, Valquíria M. H. |
author_facet |
Yoshida, Valquíria M. H. Granato, Elis Gremião, Maria Palmira Daflon Balcão, V. M. Vila, Marta M. D. C. Oliveira Junior, José M. Severino, Patrícia Souto, Eliana B. Chaud, Marco V. |
author_role |
author |
author2 |
Granato, Elis Gremião, Maria Palmira Daflon Balcão, V. M. Vila, Marta M. D. C. Oliveira Junior, José M. Severino, Patrícia Souto, Eliana B. Chaud, Marco V. |
author2_role |
author author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade do Minho |
dc.contributor.author.fl_str_mv |
Yoshida, Valquíria M. H. Granato, Elis Gremião, Maria Palmira Daflon Balcão, V. M. Vila, Marta M. D. C. Oliveira Junior, José M. Severino, Patrícia Souto, Eliana B. Chaud, Marco V. |
dc.subject.por.fl_str_mv |
3 - azidothymidine (AZT) Cal-sil floating granules Gastroretentive floating system Extended drug release Zidovudine (AZT) Polymer coating Ciências Naturais::Ciências Biológicas Ciências Médicas::Biotecnologia Médica |
topic |
3 - azidothymidine (AZT) Cal-sil floating granules Gastroretentive floating system Extended drug release Zidovudine (AZT) Polymer coating Ciências Naturais::Ciências Biológicas Ciências Médicas::Biotecnologia Médica |
description |
The aim of the research effort entertained herein was to develop, evaluate and fully characterize a multiparticulate floating gastroretentive system for the modified release of zidovudine (AZT), an antiretroviral drug. AZT was used as a water-soluble model drug at therapeutic doses. The floating gastroretentive system was obtained via polymer coating of calcium silicate-adsorbed AZT. The proposed system was evaluated in vitro for particle micromorphology, lag time for floating and duration of floating, drug loading capacity, drug release profile, and drug release kinetics. The physicochemical properties of AZT were evaluated by scanning electron microscopy (SEM) analyses, differential scanning calorimetry (DSC) analyses, X-ray diffraction (XRD) analyses, and infrared spectroscopy (FTIR) analyses. Results from SEM analysis of the AZT-containing floating gastroretentive granules allowed observation of an irregular surface and the apparent absence of pores. Floating of the AZT-containing gastroretentive granules was immediately achieved, that is lag time for floating was virtually zero and duration of floating was higher than 12 h. The drug loading capacity of the floating gastroretentive granules was ca. 81.09 ± 14.66%, and the release system thus obtained exhibited an extended drug release profile. Results from DSC and XRD analyses showed a modification in the AZT solid state, while the FTIR spectroscopy analyses revealed that the chemical structure of AZT remained unchanged upon adsorption to calcium silicate followed by polymeric coating. Hence, the coated granules produced presented gastroretentive, floating, and extended drug release properties. |
publishDate |
2013 |
dc.date.none.fl_str_mv |
2013-12 2013-12-01T00:00:00Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/1822/36850 |
url |
http://hdl.handle.net/1822/36850 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Yoshida, Valquíria M. H.; Granato, Elis; Gremião, Maria Palmira Daflon; Balcão, V. M.; Vila, Marta M. D. C.; Oliveira Junior, José M.; Severino, Patrícia; Souto, Eliana B.; Chaud, Marco V., A novel gastroretentive floating system for zidovudine, based on calcium-silicate beads. African Journal of Pharmacy and Pharmacology, 7(46), 2937-2946, 2013 1996-0816 10.5897/AJPP2013.3808 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Academic Journals |
publisher.none.fl_str_mv |
Academic Journals |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository.name.fl_str_mv |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
repository.mail.fl_str_mv |
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1799132934422134784 |