Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Detalhes bibliográficos
Autor(a) principal: Silva, Catarina M.
Data de Publicação: 2006
Outros Autores: Ribeiro, António J., Figueiredo, Isabel Vitória, Gonçalves, Alexandra Rocha, Veiga, Francisco
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10316/5747
https://doi.org/10.1016/j.ijpharm.2005.10.050
Resumo: Recombinant human insulin was encapsulated within alginate microspheres by the emulsification/internal gelation technique with the objective of preserving protein stability during encapsulation procedure. The influence of process and formulation parameters was evaluated on the morphology and encapsulation efficiency of insulin. The in vitro release of insulin from microspheres was studied under simulated gastrointestinal conditions and the in vivo activity of protein after processing was assessed by subcutaneous administration of extracted insulin from microspheres to streptozotocin-induced diabetic rats. Microspheres mean diameter, ranging from 21 to 287 [mu]m, decreased with the internal phase ratio, emulsifier concentration, mixer rotational speed and increased with alginate concentration. Insulin encapsulation efficiency, near 75%, was not affected by emulsifier concentration, mixer rotational speed and zinc/insulin hexamer molar ratio but decreased either by increasing internal phase ratio and calcium/alginate mass ratio or by decreasing acid/calcium molar ratio and alginate concentration. A high insulin release, above 75%, was obtained at pH 1.2 and under simulated intestinal pH a complete dissolution of microspheres occurred. Extracted insulin from microspheres decreased hyperglycemia of diabetic rats proving to be bioactive and showing that encapsulation in alginate microspheres using the emulsification/internal gelation is an appropriate method for protein encapsulation.
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spelling Alginate microspheres prepared by internal gelation: Development and effect on insulin stabilityAlginateBioactivityInsulinInternal gelationMicrospheresRecombinant human insulin was encapsulated within alginate microspheres by the emulsification/internal gelation technique with the objective of preserving protein stability during encapsulation procedure. The influence of process and formulation parameters was evaluated on the morphology and encapsulation efficiency of insulin. The in vitro release of insulin from microspheres was studied under simulated gastrointestinal conditions and the in vivo activity of protein after processing was assessed by subcutaneous administration of extracted insulin from microspheres to streptozotocin-induced diabetic rats. Microspheres mean diameter, ranging from 21 to 287 [mu]m, decreased with the internal phase ratio, emulsifier concentration, mixer rotational speed and increased with alginate concentration. Insulin encapsulation efficiency, near 75%, was not affected by emulsifier concentration, mixer rotational speed and zinc/insulin hexamer molar ratio but decreased either by increasing internal phase ratio and calcium/alginate mass ratio or by decreasing acid/calcium molar ratio and alginate concentration. A high insulin release, above 75%, was obtained at pH 1.2 and under simulated intestinal pH a complete dissolution of microspheres occurred. Extracted insulin from microspheres decreased hyperglycemia of diabetic rats proving to be bioactive and showing that encapsulation in alginate microspheres using the emulsification/internal gelation is an appropriate method for protein encapsulation.http://www.sciencedirect.com/science/article/B6T7W-4J4B994-3/1/737714c13ec0b481ae55c4c1c319f3e12006info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleaplication/PDFhttp://hdl.handle.net/10316/5747http://hdl.handle.net/10316/5747https://doi.org/10.1016/j.ijpharm.2005.10.050engInternational Journal of Pharmaceutics. 311:1-2 (2006) 1-10Silva, Catarina M.Ribeiro, António J.Figueiredo, Isabel VitóriaGonçalves, Alexandra RochaVeiga, Franciscoinfo: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:RCAAP2020-11-06T16:49:07Zoai:estudogeral.uc.pt:10316/5747Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:47:17.252060Repositório 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 Alginate microspheres prepared by internal gelation: Development and effect on insulin stability
title Alginate microspheres prepared by internal gelation: Development and effect on insulin stability
spellingShingle Alginate microspheres prepared by internal gelation: Development and effect on insulin stability
Silva, Catarina M.
Alginate
Bioactivity
Insulin
Internal gelation
Microspheres
title_short Alginate microspheres prepared by internal gelation: Development and effect on insulin stability
title_full Alginate microspheres prepared by internal gelation: Development and effect on insulin stability
title_fullStr Alginate microspheres prepared by internal gelation: Development and effect on insulin stability
title_full_unstemmed Alginate microspheres prepared by internal gelation: Development and effect on insulin stability
title_sort Alginate microspheres prepared by internal gelation: Development and effect on insulin stability
author Silva, Catarina M.
author_facet Silva, Catarina M.
Ribeiro, António J.
Figueiredo, Isabel Vitória
Gonçalves, Alexandra Rocha
Veiga, Francisco
author_role author
author2 Ribeiro, António J.
Figueiredo, Isabel Vitória
Gonçalves, Alexandra Rocha
Veiga, Francisco
author2_role author
author
author
author
dc.contributor.author.fl_str_mv Silva, Catarina M.
Ribeiro, António J.
Figueiredo, Isabel Vitória
Gonçalves, Alexandra Rocha
Veiga, Francisco
dc.subject.por.fl_str_mv Alginate
Bioactivity
Insulin
Internal gelation
Microspheres
topic Alginate
Bioactivity
Insulin
Internal gelation
Microspheres
description Recombinant human insulin was encapsulated within alginate microspheres by the emulsification/internal gelation technique with the objective of preserving protein stability during encapsulation procedure. The influence of process and formulation parameters was evaluated on the morphology and encapsulation efficiency of insulin. The in vitro release of insulin from microspheres was studied under simulated gastrointestinal conditions and the in vivo activity of protein after processing was assessed by subcutaneous administration of extracted insulin from microspheres to streptozotocin-induced diabetic rats. Microspheres mean diameter, ranging from 21 to 287 [mu]m, decreased with the internal phase ratio, emulsifier concentration, mixer rotational speed and increased with alginate concentration. Insulin encapsulation efficiency, near 75%, was not affected by emulsifier concentration, mixer rotational speed and zinc/insulin hexamer molar ratio but decreased either by increasing internal phase ratio and calcium/alginate mass ratio or by decreasing acid/calcium molar ratio and alginate concentration. A high insulin release, above 75%, was obtained at pH 1.2 and under simulated intestinal pH a complete dissolution of microspheres occurred. Extracted insulin from microspheres decreased hyperglycemia of diabetic rats proving to be bioactive and showing that encapsulation in alginate microspheres using the emulsification/internal gelation is an appropriate method for protein encapsulation.
publishDate 2006
dc.date.none.fl_str_mv 2006
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dc.identifier.uri.fl_str_mv http://hdl.handle.net/10316/5747
http://hdl.handle.net/10316/5747
https://doi.org/10.1016/j.ijpharm.2005.10.050
url http://hdl.handle.net/10316/5747
https://doi.org/10.1016/j.ijpharm.2005.10.050
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv International Journal of Pharmaceutics. 311:1-2 (2006) 1-10
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