Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response

Detalhes bibliográficos
Autor(a) principal: Reis, Catarina P.
Data de Publicação: 2008
Outros Autores: Veiga, Francisco J., Ribeiro, António J., Neufeld, Ronald J., Damgé, Christiane
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10316/8354
https://doi.org/10.1002/jps.21347
Resumo: The aim of this study was to characterize and evaluate a novel oral insulin nanoparticulate system based on alginate-dextran sulfate core, complexed with a chitosan-polyethylene glycol-albumin shell. Insulin-loaded nanospheres (25, 50, 100 IU/kg) administered orally to diabetic rats reduced glycemia in a dose dependent manner. This effect lasted over 24 h with a maximal effect after 14 h. Nanospheres increased insulin plasma level and improved glycemic response to an oral glucose overload. After 4 days oral administration (50 IU/kg/day), the metabolic status of diabetic rats improved with a reduction in water intake, urine excretion and proteinuria. FITC-insulin-loaded nanospheres administered to an isolated intestinal loop were taken up by the intestinal mucosa. They strongly adhered to villus apical enterocytes and markedly labeled Peyer's patches. It is concluded that nanospheres preserve insulin and exert an antidiabetic effect after oral administration. This is explained by a protective effect against proteolytic enzymes by the albumin coating, by the mucoadhesive properties of chitosan-polyethylene glycol, and by the possibility of chitosan reversibly altering tight junctions leading to an improved absorption of insulin. This formulation demonstrates beneficial effects on diabetic symptoms and will be of interest in the treatment of diabetes with oral insulin. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci
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spelling Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological responseThe aim of this study was to characterize and evaluate a novel oral insulin nanoparticulate system based on alginate-dextran sulfate core, complexed with a chitosan-polyethylene glycol-albumin shell. Insulin-loaded nanospheres (25, 50, 100 IU/kg) administered orally to diabetic rats reduced glycemia in a dose dependent manner. This effect lasted over 24 h with a maximal effect after 14 h. Nanospheres increased insulin plasma level and improved glycemic response to an oral glucose overload. After 4 days oral administration (50 IU/kg/day), the metabolic status of diabetic rats improved with a reduction in water intake, urine excretion and proteinuria. FITC-insulin-loaded nanospheres administered to an isolated intestinal loop were taken up by the intestinal mucosa. They strongly adhered to villus apical enterocytes and markedly labeled Peyer's patches. It is concluded that nanospheres preserve insulin and exert an antidiabetic effect after oral administration. This is explained by a protective effect against proteolytic enzymes by the albumin coating, by the mucoadhesive properties of chitosan-polyethylene glycol, and by the possibility of chitosan reversibly altering tight junctions leading to an improved absorption of insulin. This formulation demonstrates beneficial effects on diabetic symptoms and will be of interest in the treatment of diabetes with oral insulin. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci2008info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/8354http://hdl.handle.net/10316/8354https://doi.org/10.1002/jps.21347engJournal of Pharmaceutical Sciences. 9999:9999 (2008) n/aReis, Catarina P.Veiga, Francisco J.Ribeiro, António J.Neufeld, Ronald J.Damgé, Christianeinfo: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:RCAAP2021-11-08T11:14:41Zoai:estudogeral.uc.pt:10316/8354Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:47:20.946168Repositório 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 Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response
title Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response
spellingShingle Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response
Reis, Catarina P.
title_short Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response
title_full Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response
title_fullStr Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response
title_full_unstemmed Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response
title_sort Nanoparticulate biopolymers deliver insulin orally eliciting pharmacological response
author Reis, Catarina P.
author_facet Reis, Catarina P.
Veiga, Francisco J.
Ribeiro, António J.
Neufeld, Ronald J.
Damgé, Christiane
author_role author
author2 Veiga, Francisco J.
Ribeiro, António J.
Neufeld, Ronald J.
Damgé, Christiane
author2_role author
author
author
author
dc.contributor.author.fl_str_mv Reis, Catarina P.
Veiga, Francisco J.
Ribeiro, António J.
Neufeld, Ronald J.
Damgé, Christiane
description The aim of this study was to characterize and evaluate a novel oral insulin nanoparticulate system based on alginate-dextran sulfate core, complexed with a chitosan-polyethylene glycol-albumin shell. Insulin-loaded nanospheres (25, 50, 100 IU/kg) administered orally to diabetic rats reduced glycemia in a dose dependent manner. This effect lasted over 24 h with a maximal effect after 14 h. Nanospheres increased insulin plasma level and improved glycemic response to an oral glucose overload. After 4 days oral administration (50 IU/kg/day), the metabolic status of diabetic rats improved with a reduction in water intake, urine excretion and proteinuria. FITC-insulin-loaded nanospheres administered to an isolated intestinal loop were taken up by the intestinal mucosa. They strongly adhered to villus apical enterocytes and markedly labeled Peyer's patches. It is concluded that nanospheres preserve insulin and exert an antidiabetic effect after oral administration. This is explained by a protective effect against proteolytic enzymes by the albumin coating, by the mucoadhesive properties of chitosan-polyethylene glycol, and by the possibility of chitosan reversibly altering tight junctions leading to an improved absorption of insulin. This formulation demonstrates beneficial effects on diabetic symptoms and will be of interest in the treatment of diabetes with oral insulin. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci
publishDate 2008
dc.date.none.fl_str_mv 2008
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
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dc.identifier.uri.fl_str_mv http://hdl.handle.net/10316/8354
http://hdl.handle.net/10316/8354
https://doi.org/10.1002/jps.21347
url http://hdl.handle.net/10316/8354
https://doi.org/10.1002/jps.21347
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Journal of Pharmaceutical Sciences. 9999:9999 (2008) n/a
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