New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells
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/10316/25649 https://doi.org/10.3109/03639045.2012.669129 |
Resumo: | Objective: The aim of this study was to adjust the zidovudine (AZT) release from solid tablets to an ideal profile, by developing matrices comprising swellable polymers with nonswellable ones. Methods: Directly compressed matrices comprised different ratios of hydroxypropylmethylcellulose K15M and K100M, ethylcellulose, and methacrylic acid (Eudragit® RS PO and Eudragit® RL PO) were prepared. Technological characterization and evaluation of the in vitro release behavior were carried out. Cell density and viability following drug exposure were evaluated by the SRB method, for the Caco-2 line, while cell morphology was assessed upon Trypan blue staining. Results: A specific formulation containing 5% of each excipient − HPMC K15M, HPMC K100M, Eudragit® RS PO, and Eudragit® RL PO − was found to yield the best release profile. Application of the Korsmeyer–Peppas model to the dissolution profile evidenced that a non-Fickian (anomalous) transport is involved in the drug release. Regarding the influence of the tablets’ composition on the drug’s cytotoxic effect toward the Caco-2 cell line, a reduction of cell biomass (0–15%) was verified for the distinct AZT formulations tested, F19 having displayed the highest cytotoxicity, after 24 and 48 h of incubation. Additionally, a high reversibility of the AZT effect was observed. Conclusions: The results showed that the simultaneous application of both hydrophilic and hydrophobic polymers can modulate the drug release process, leading to an improved efficacy and patient compliance. All AZT formulations studied were found to be cytotoxic against Caco-2 cells, F19 being the most effective one. |
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New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cellsZidovudine (AZT)hydroxypropylmethylcellulose (HPMC)Eudragit®in vitro releaseantiproliferative effectRaman spectroscopyObjective: The aim of this study was to adjust the zidovudine (AZT) release from solid tablets to an ideal profile, by developing matrices comprising swellable polymers with nonswellable ones. Methods: Directly compressed matrices comprised different ratios of hydroxypropylmethylcellulose K15M and K100M, ethylcellulose, and methacrylic acid (Eudragit® RS PO and Eudragit® RL PO) were prepared. Technological characterization and evaluation of the in vitro release behavior were carried out. Cell density and viability following drug exposure were evaluated by the SRB method, for the Caco-2 line, while cell morphology was assessed upon Trypan blue staining. Results: A specific formulation containing 5% of each excipient − HPMC K15M, HPMC K100M, Eudragit® RS PO, and Eudragit® RL PO − was found to yield the best release profile. Application of the Korsmeyer–Peppas model to the dissolution profile evidenced that a non-Fickian (anomalous) transport is involved in the drug release. Regarding the influence of the tablets’ composition on the drug’s cytotoxic effect toward the Caco-2 cell line, a reduction of cell biomass (0–15%) was verified for the distinct AZT formulations tested, F19 having displayed the highest cytotoxicity, after 24 and 48 h of incubation. Additionally, a high reversibility of the AZT effect was observed. Conclusions: The results showed that the simultaneous application of both hydrophilic and hydrophobic polymers can modulate the drug release process, leading to an improved efficacy and patient compliance. All AZT formulations studied were found to be cytotoxic against Caco-2 cells, F19 being the most effective one.J.V.S. acknowledges PhD fellowship from the Programme Alβan, the European Union Programme of High Level Scholarships for Latin America (scholarship no. E06D100103BR).Informa Healthcare2013info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/25649http://hdl.handle.net/10316/25649https://doi.org/10.3109/03639045.2012.669129enghttp://informahealthcare.com/doi/abs/10.3109/03639045.2012.669129Santos, Jucimary V.Pina, Maria Eugénia T.Marques, M. P. M.Carvalho, Luís A. E. Batista deinfo: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:RCAAP2021-11-05T12:39:09Zoai:estudogeral.uc.pt:10316/25649Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:56:04.632847Repositório 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 |
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells |
title |
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells |
spellingShingle |
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells Santos, Jucimary V. Zidovudine (AZT) hydroxypropylmethylcellulose (HPMC) Eudragit® in vitro release antiproliferative effect Raman spectroscopy |
title_short |
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells |
title_full |
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells |
title_fullStr |
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells |
title_full_unstemmed |
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells |
title_sort |
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells |
author |
Santos, Jucimary V. |
author_facet |
Santos, Jucimary V. Pina, Maria Eugénia T. Marques, M. P. M. Carvalho, Luís A. E. Batista de |
author_role |
author |
author2 |
Pina, Maria Eugénia T. Marques, M. P. M. Carvalho, Luís A. E. Batista de |
author2_role |
author author author |
dc.contributor.author.fl_str_mv |
Santos, Jucimary V. Pina, Maria Eugénia T. Marques, M. P. M. Carvalho, Luís A. E. Batista de |
dc.subject.por.fl_str_mv |
Zidovudine (AZT) hydroxypropylmethylcellulose (HPMC) Eudragit® in vitro release antiproliferative effect Raman spectroscopy |
topic |
Zidovudine (AZT) hydroxypropylmethylcellulose (HPMC) Eudragit® in vitro release antiproliferative effect Raman spectroscopy |
description |
Objective: The aim of this study was to adjust the zidovudine (AZT) release from solid tablets to an ideal profile, by developing matrices comprising swellable polymers with nonswellable ones. Methods: Directly compressed matrices comprised different ratios of hydroxypropylmethylcellulose K15M and K100M, ethylcellulose, and methacrylic acid (Eudragit® RS PO and Eudragit® RL PO) were prepared. Technological characterization and evaluation of the in vitro release behavior were carried out. Cell density and viability following drug exposure were evaluated by the SRB method, for the Caco-2 line, while cell morphology was assessed upon Trypan blue staining. Results: A specific formulation containing 5% of each excipient − HPMC K15M, HPMC K100M, Eudragit® RS PO, and Eudragit® RL PO − was found to yield the best release profile. Application of the Korsmeyer–Peppas model to the dissolution profile evidenced that a non-Fickian (anomalous) transport is involved in the drug release. Regarding the influence of the tablets’ composition on the drug’s cytotoxic effect toward the Caco-2 cell line, a reduction of cell biomass (0–15%) was verified for the distinct AZT formulations tested, F19 having displayed the highest cytotoxicity, after 24 and 48 h of incubation. Additionally, a high reversibility of the AZT effect was observed. Conclusions: The results showed that the simultaneous application of both hydrophilic and hydrophobic polymers can modulate the drug release process, leading to an improved efficacy and patient compliance. All AZT formulations studied were found to be cytotoxic against Caco-2 cells, F19 being the most effective one. |
publishDate |
2013 |
dc.date.none.fl_str_mv |
2013 |
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/10316/25649 http://hdl.handle.net/10316/25649 https://doi.org/10.3109/03639045.2012.669129 |
url |
http://hdl.handle.net/10316/25649 https://doi.org/10.3109/03639045.2012.669129 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
http://informahealthcare.com/doi/abs/10.3109/03639045.2012.669129 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.publisher.none.fl_str_mv |
Informa Healthcare |
publisher.none.fl_str_mv |
Informa Healthcare |
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 |
instacron_str |
RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
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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1799133846081372160 |