Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers

Detalhes bibliográficos
Autor(a) principal: Natu, Mădălina V.
Data de Publicação: 2010
Outros Autores: Sousa, Hermínio C. de, Gil, M. H.
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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spelling 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)
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collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
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