Nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery

Lei Song, Zheng-liang Zhi, John C PickupDiabetes Research Group, King's College London School of Medicine, Guy's Hospital, London, United KingdomAbstract: Current oral insulin formulations reported in the literature are often associated with an unpredictable burst release of insulin...

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Autores principales:	Song L, Zhi ZL, Pickup JC
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/ac8e669dc4684f9a903a1023e15fd263
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spelling	oai:doaj.org-article:ac8e669dc4684f9a903a1023e15fd2632021-12-02T02:21:12ZNanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery1178-2013https://doaj.org/article/ac8e669dc4684f9a903a1023e15fd2632014-05-01T00:00:00Zhttp://www.dovepress.com/nanolayer-encapsulation-of-insulin--chitosan-complexes-improves-effici-a16632https://doaj.org/toc/1178-2013 Lei Song, Zheng-liang Zhi, John C PickupDiabetes Research Group, King's College London School of Medicine, Guy's Hospital, London, United KingdomAbstract: Current oral insulin formulations reported in the literature are often associated with an unpredictable burst release of insulin in the intestine, which may increase the risk for problematic hypoglycemia. The aim of the study was to develop a solution based on a nanolayer encapsulation of insulin-chitosan complexes to afford sustained release after oral administration. Chitosan/heparin multilayer coatings were deposited onto insulin-chitosan microparticulate cores in the presence of poly(ethylene) glycol (PEG) in the precipitating and coating solutions. The addition of PEG improved insulin loading and minimized an undesirable loss of the protein resulting from redissolution. Nanolayer encapsulation and the formation of complexes enabled a superior loading capacity of insulin (>90%), as well as enhanced stability and 74% decreased solubility at acid pH in vitro, compared with nonencapsulated insulin. The capsulated insulin administered by oral gavage lowered fasting blood glucose levels by up to 50% in a sustained and dose-dependent manner and reduced postprandial glycemia in streptozotocin-induced diabetic mice without causing hypoglycemia. Nanolayer encapsulation reduced the possibility of rapid and erratic falls of blood glucose levels in animals. This technique represents a promising strategy to promote the intestinal absorption efficiency and release behavior of the hormone, potentially enabling an efficient and safe route for oral insulin delivery of insulin in diabetes management.Keywords: oral insulin, diabetes mellitus, insulin-chitosan complexes, multilayer nanoencapsulation, polyethylene glycol, chitosan, heparinSong LZhi ZLPickup JCDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 2127-2136 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Song L Zhi ZL Pickup JC Nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery
description	Lei Song, Zheng-liang Zhi, John C PickupDiabetes Research Group, King's College London School of Medicine, Guy's Hospital, London, United KingdomAbstract: Current oral insulin formulations reported in the literature are often associated with an unpredictable burst release of insulin in the intestine, which may increase the risk for problematic hypoglycemia. The aim of the study was to develop a solution based on a nanolayer encapsulation of insulin-chitosan complexes to afford sustained release after oral administration. Chitosan/heparin multilayer coatings were deposited onto insulin-chitosan microparticulate cores in the presence of poly(ethylene) glycol (PEG) in the precipitating and coating solutions. The addition of PEG improved insulin loading and minimized an undesirable loss of the protein resulting from redissolution. Nanolayer encapsulation and the formation of complexes enabled a superior loading capacity of insulin (>90%), as well as enhanced stability and 74% decreased solubility at acid pH in vitro, compared with nonencapsulated insulin. The capsulated insulin administered by oral gavage lowered fasting blood glucose levels by up to 50% in a sustained and dose-dependent manner and reduced postprandial glycemia in streptozotocin-induced diabetic mice without causing hypoglycemia. Nanolayer encapsulation reduced the possibility of rapid and erratic falls of blood glucose levels in animals. This technique represents a promising strategy to promote the intestinal absorption efficiency and release behavior of the hormone, potentially enabling an efficient and safe route for oral insulin delivery of insulin in diabetes management.Keywords: oral insulin, diabetes mellitus, insulin-chitosan complexes, multilayer nanoencapsulation, polyethylene glycol, chitosan, heparin
format	article
author	Song L Zhi ZL Pickup JC
author_facet	Song L Zhi ZL Pickup JC
author_sort	Song L
title	Nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery
title_short	Nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery
title_full	Nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery
title_fullStr	Nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery
title_full_unstemmed	Nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery
title_sort	nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/ac8e669dc4684f9a903a1023e15fd263
work_keys_str_mv	AT songl nanolayerencapsulationofinsulinchitosancomplexesimprovesefficiencyoforalinsulindelivery AT zhizl nanolayerencapsulationofinsulinchitosancomplexesimprovesefficiencyoforalinsulindelivery AT pickupjc nanolayerencapsulationofinsulinchitosancomplexesimprovesefficiencyoforalinsulindelivery
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Nanolayer encapsulation of insulin- chitosan complexes improves efficiency of oral insulin delivery

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