Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers
Autor(a) principal: | |
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Data de Publicação: | 2010 |
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/10316/21648 https://doi.org/10.1016/j.ijpharm.2010.06.045 |
Resumo: | Bicomponent fibers of two semi-crystalline (co)polymers, poly(ɛ-caprolactone), and poly(oxyethylene-b-oxypropylene-b-oxyethylene), were obtained by electrospinning. Acetazolamide and timolol maleate were loaded in the fibers in different concentrations (below and above the drug solubility limit in polymer) in order to determine the effect of drug solubility in polymer, drug state, drug loading and fiber composition on fiber morphology, drug distribution and release kinetics. The high loadings fibers (with drug in crystalline form) showed higher burst and faster release than low drug content fibers, indicating the release was more sustained when the drug was encapsulated inside the fibers, in amorphous form. Moreover, timolol maleate was released faster than acetazolamide, indicating that drug solubility in polymer influences the partition of drug between polymer and elution medium, while fiber composition also controlled drug release. At low loadings, total release was not achieved (cumulative release percentages smaller than 100%), suggesting that drug remained trapped in the fibers. The modeling of release data implied a three stage release mechanism: a dissolution stage, a desorption and subsequent diffusion through water-filled pores, followed by polymer degradation control. |
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Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibersElectrospinningBicomponent fibersDrug releaseModelingBicomponent fibers of two semi-crystalline (co)polymers, poly(ɛ-caprolactone), and poly(oxyethylene-b-oxypropylene-b-oxyethylene), were obtained by electrospinning. Acetazolamide and timolol maleate were loaded in the fibers in different concentrations (below and above the drug solubility limit in polymer) in order to determine the effect of drug solubility in polymer, drug state, drug loading and fiber composition on fiber morphology, drug distribution and release kinetics. The high loadings fibers (with drug in crystalline form) showed higher burst and faster release than low drug content fibers, indicating the release was more sustained when the drug was encapsulated inside the fibers, in amorphous form. Moreover, timolol maleate was released faster than acetazolamide, indicating that drug solubility in polymer influences the partition of drug between polymer and elution medium, while fiber composition also controlled drug release. At low loadings, total release was not achieved (cumulative release percentages smaller than 100%), suggesting that drug remained trapped in the fibers. The modeling of release data implied a three stage release mechanism: a dissolution stage, a desorption and subsequent diffusion through water-filled pores, followed by polymer degradation control.Elsevier2010-09info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/21648http://hdl.handle.net/10316/21648https://doi.org/10.1016/j.ijpharm.2010.06.045engNATU, Mădălina V.; SOUSA, Hermínio C. de; GIL, M. H. - Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers. "International Journal of Pharmaceutics". ISSN 0378-5173. 397:1–2 (2010) 50–580378-5173http://www.sciencedirect.com/science/article/pii/S0378517310005028Natu, Mădălina V.Sousa, Hermínio C. deGil, M. H.info: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:RCAAP2020-05-29T09:42:39Zoai:estudogeral.uc.pt:10316/21648Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:59:21.483477Repositório 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 |
Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers |
title |
Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers |
spellingShingle |
Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers Natu, Mădălina V. Electrospinning Bicomponent fibers Drug release Modeling |
title_short |
Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers |
title_full |
Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers |
title_fullStr |
Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers |
title_full_unstemmed |
Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers |
title_sort |
Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers |
author |
Natu, Mădălina V. |
author_facet |
Natu, Mădălina V. Sousa, Hermínio C. de Gil, M. H. |
author_role |
author |
author2 |
Sousa, Hermínio C. de Gil, M. H. |
author2_role |
author author |
dc.contributor.author.fl_str_mv |
Natu, Mădălina V. Sousa, Hermínio C. de Gil, M. H. |
dc.subject.por.fl_str_mv |
Electrospinning Bicomponent fibers Drug release Modeling |
topic |
Electrospinning Bicomponent fibers Drug release Modeling |
description |
Bicomponent fibers of two semi-crystalline (co)polymers, poly(ɛ-caprolactone), and poly(oxyethylene-b-oxypropylene-b-oxyethylene), were obtained by electrospinning. Acetazolamide and timolol maleate were loaded in the fibers in different concentrations (below and above the drug solubility limit in polymer) in order to determine the effect of drug solubility in polymer, drug state, drug loading and fiber composition on fiber morphology, drug distribution and release kinetics. The high loadings fibers (with drug in crystalline form) showed higher burst and faster release than low drug content fibers, indicating the release was more sustained when the drug was encapsulated inside the fibers, in amorphous form. Moreover, timolol maleate was released faster than acetazolamide, indicating that drug solubility in polymer influences the partition of drug between polymer and elution medium, while fiber composition also controlled drug release. At low loadings, total release was not achieved (cumulative release percentages smaller than 100%), suggesting that drug remained trapped in the fibers. The modeling of release data implied a three stage release mechanism: a dissolution stage, a desorption and subsequent diffusion through water-filled pores, followed by polymer degradation control. |
publishDate |
2010 |
dc.date.none.fl_str_mv |
2010-09 |
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/10316/21648 http://hdl.handle.net/10316/21648 https://doi.org/10.1016/j.ijpharm.2010.06.045 |
url |
http://hdl.handle.net/10316/21648 https://doi.org/10.1016/j.ijpharm.2010.06.045 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
NATU, Mădălina V.; SOUSA, Hermínio C. de; GIL, M. H. - Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers. "International Journal of Pharmaceutics". ISSN 0378-5173. 397:1–2 (2010) 50–58 0378-5173 http://www.sciencedirect.com/science/article/pii/S0378517310005028 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.publisher.none.fl_str_mv |
Elsevier |
publisher.none.fl_str_mv |
Elsevier |
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 |
institution |
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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1799133885307551744 |