Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process
Autor(a) principal: | |
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Data de Publicação: | 2015 |
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/1822/35310 |
Resumo: | A supercritical antisolvent (SAS) process for obtaining zidovudine-poly(l-lactic acid) (PLLA) solid dispersions (SDs) was used to attain a better intestinal permeation of this drug. A 32 factorial design was used, having as independent variables the ratio 3-azido-23-dideoxythymidine (AZT)PLLA and temperature/pressure conditions, as dependent variables the process yield and particle macroscopic morphology. AZTPLLA production batches were carried out by the SAS process, and the resulting products evaluated via scanning electron microscope, X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared analyses. From the nine possible combinations of tests performed experimentally, only one combination did not produced a solid. The L3 batch of SD, produced with 1:2 (AZTPLLA) ratio, resulted in a 91.54% yield, with 40% AZT content. Intestinal permeability studies using the AZTPLLA from L3 batch led to an AZT permeability of approximately 9.87%, which was higher than that of pure AZT (3.84%). AZT remained in crystalline form, whereas PLLA remained in semicrystalline form. AZT release is controlled by a diffusion mechanism. It has been demonstrated that it is possible to use PLLA carrier and SAS process to obtain SD, in a single step. |
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Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent processsupercritical antisolvent processsupercritical fluidszidovudinepoly(l-lactic acid)solid dispersionoral absorptiongastrointestinal transiteverted rat intestinal sacspermeabilityCiências Médicas::Biotecnologia MédicaScience & TechnologyA supercritical antisolvent (SAS) process for obtaining zidovudine-poly(l-lactic acid) (PLLA) solid dispersions (SDs) was used to attain a better intestinal permeation of this drug. A 32 factorial design was used, having as independent variables the ratio 3-azido-23-dideoxythymidine (AZT)PLLA and temperature/pressure conditions, as dependent variables the process yield and particle macroscopic morphology. AZTPLLA production batches were carried out by the SAS process, and the resulting products evaluated via scanning electron microscope, X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared analyses. From the nine possible combinations of tests performed experimentally, only one combination did not produced a solid. The L3 batch of SD, produced with 1:2 (AZTPLLA) ratio, resulted in a 91.54% yield, with 40% AZT content. Intestinal permeability studies using the AZTPLLA from L3 batch led to an AZT permeability of approximately 9.87%, which was higher than that of pure AZT (3.84%). AZT remained in crystalline form, whereas PLLA remained in semicrystalline form. AZT release is controlled by a diffusion mechanism. It has been demonstrated that it is possible to use PLLA carrier and SAS process to obtain SD, in a single step.Cristalia (Itapira, Brazil) for the kind supply of the reference substance used throughout the research work. Financial support from Fundação de Amparo á Pesquisa do Estado de São Paulo (2013-19300-4; 2012/01333-0; 2011/21219-5), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (PROSUP/CAPES) and Finep Inovação e Pesquisa (Finep, Brazil; 01.13.0286.00).John Wiley and SonsUniversidade do MinhoYoshida, Valquíria M. H.Balcão, V. M.Vila, Marta M. D. C.Oliveira Júnior, J. M.Aranha, NorbertoChaud, Marco V.Gremião, Maria P. D.2015-052015-05-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/1822/35310engYoshida, Valquíria M. H.; Balcão, V. M.; Vila, Marta M. D. C.; Oliveira Júnior, José M.; Aranha, Norberto; Chaud, Marco V.; Gremião, Maria P. D., Zidovudinepoly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process. Journal of Pharmaceutical Sciences, 104(5), 1691-1700, 20150022-35491520-601710.1002/jps.2437725676038http://onlinelibrary.wiley.com/doi/10.1002/jps.24377/abstractinfo: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:RCAAP2023-07-21T12:24:34Zoai:repositorium.sdum.uminho.pt:1822/35310Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T19:18:36.353514Repositório 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 |
Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process |
title |
Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process |
spellingShingle |
Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process Yoshida, Valquíria M. H. supercritical antisolvent process supercritical fluids zidovudine poly(l-lactic acid) solid dispersion oral absorption gastrointestinal transit everted rat intestinal sacs permeability Ciências Médicas::Biotecnologia Médica Science & Technology |
title_short |
Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process |
title_full |
Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process |
title_fullStr |
Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process |
title_full_unstemmed |
Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process |
title_sort |
Zidovudine-poly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process |
author |
Yoshida, Valquíria M. H. |
author_facet |
Yoshida, Valquíria M. H. Balcão, V. M. Vila, Marta M. D. C. Oliveira Júnior, J. M. Aranha, Norberto Chaud, Marco V. Gremião, Maria P. D. |
author_role |
author |
author2 |
Balcão, V. M. Vila, Marta M. D. C. Oliveira Júnior, J. M. Aranha, Norberto Chaud, Marco V. Gremião, Maria P. D. |
author2_role |
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. Balcão, V. M. Vila, Marta M. D. C. Oliveira Júnior, J. M. Aranha, Norberto Chaud, Marco V. Gremião, Maria P. D. |
dc.subject.por.fl_str_mv |
supercritical antisolvent process supercritical fluids zidovudine poly(l-lactic acid) solid dispersion oral absorption gastrointestinal transit everted rat intestinal sacs permeability Ciências Médicas::Biotecnologia Médica Science & Technology |
topic |
supercritical antisolvent process supercritical fluids zidovudine poly(l-lactic acid) solid dispersion oral absorption gastrointestinal transit everted rat intestinal sacs permeability Ciências Médicas::Biotecnologia Médica Science & Technology |
description |
A supercritical antisolvent (SAS) process for obtaining zidovudine-poly(l-lactic acid) (PLLA) solid dispersions (SDs) was used to attain a better intestinal permeation of this drug. A 32 factorial design was used, having as independent variables the ratio 3-azido-23-dideoxythymidine (AZT)PLLA and temperature/pressure conditions, as dependent variables the process yield and particle macroscopic morphology. AZTPLLA production batches were carried out by the SAS process, and the resulting products evaluated via scanning electron microscope, X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared analyses. From the nine possible combinations of tests performed experimentally, only one combination did not produced a solid. The L3 batch of SD, produced with 1:2 (AZTPLLA) ratio, resulted in a 91.54% yield, with 40% AZT content. Intestinal permeability studies using the AZTPLLA from L3 batch led to an AZT permeability of approximately 9.87%, which was higher than that of pure AZT (3.84%). AZT remained in crystalline form, whereas PLLA remained in semicrystalline form. AZT release is controlled by a diffusion mechanism. It has been demonstrated that it is possible to use PLLA carrier and SAS process to obtain SD, in a single step. |
publishDate |
2015 |
dc.date.none.fl_str_mv |
2015-05 2015-05-01T00:00:00Z |
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/1822/35310 |
url |
http://hdl.handle.net/1822/35310 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Yoshida, Valquíria M. H.; Balcão, V. M.; Vila, Marta M. D. C.; Oliveira Júnior, José M.; Aranha, Norberto; Chaud, Marco V.; Gremião, Maria P. D., Zidovudinepoly(l-lactic acid) solid dispersions with improved intestinal permeability prepared by supercritical antisolvent process. Journal of Pharmaceutical Sciences, 104(5), 1691-1700, 2015 0022-3549 1520-6017 10.1002/jps.24377 25676038 http://onlinelibrary.wiley.com/doi/10.1002/jps.24377/abstract |
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 |
John Wiley and Sons |
publisher.none.fl_str_mv |
John Wiley and Sons |
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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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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