Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats

Xiaoyang Li, Jianping Qi, Yunchang Xie, Xi Zhang, Shunwen Hu, Ying Xu, Yi Lu, Wei WuKey Laboratory of Smart Drug Delivery of Ministry of Education and People&#39;s Liberation Army (PLA), School of Pharmacy, Fudan University, Shanghai, ChinaAbstract: This study aimed to prepare nanoemulsions...

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Autores principales:	Li X, Qi J, Xie Y, Zhang X, Hu S, Xu Y, Lu Y, Wu W
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/f030047e68354f13a5c1d4dd1ac9f685
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spelling	oai:doaj.org-article:f030047e68354f13a5c1d4dd1ac9f6852021-12-02T01:50:41ZNanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats1176-91141178-2013https://doaj.org/article/f030047e68354f13a5c1d4dd1ac9f6852012-12-01T00:00:00Zhttp://www.dovepress.com/nanoemulsions-coated-with-alginatechitosan-as-oral-insulin-delivery-sy-a11832https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Xiaoyang Li, Jianping Qi, Yunchang Xie, Xi Zhang, Shunwen Hu, Ying Xu, Yi Lu, Wei WuKey Laboratory of Smart Drug Delivery of Ministry of Education and People&#39;s Liberation Army (PLA), School of Pharmacy, Fudan University, Shanghai, ChinaAbstract: This study aimed to prepare nanoemulsions coated with alginate/chitosan for oral insulin delivery. Uncoated nanoemulsions were prepared by homogenization of a water in oil in water (w/o/w) multiple emulsion that was composed of Labrafac&reg; CC, phospholipid, Span&trade; 80 and Cremorphor&reg; EL. Coating of the nanoemulsions was achieved based on polyelectrolyte cross-linking, with sequential addition of calcium chloride and chitosan to the bulk nanoemulsion dispersion that contained alginate. The particle size of the coated nanoemulsions was about 488 nm and the insulin entrapment ratio was 47.3%. Circular dichroism spectroscopy proved conformational stability of insulin against the preparative stress. In vitro leakage study indicated well-preserved integrity of the nanoemulsions in simulated gastric juices. Hypoglycemic effects were observed in both normal and diabetic rats. The relative pharmacological bioavailability of the coated nanoemulsion with 25 and 50 IU/kg insulin were 8.42% and 5.72% in normal rats and 8.19% and 7.84% in diabetic rats, respectively. Moreover, there were significantly prolonged hypoglycemic effects after oral administration of the coated nanoemulsions compared with subcutaneous (sc) insulin. In conclusion, the nanoemulsion coated with alginate/chitosan was a potential delivery system for oral delivery of polypeptides and proteins.Keywords: insulin, oral delivery, alginate, chitosan, nanoemulsionLi XQi JXie YZhang XHu SXu YLu YWu WDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 23-32 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Li X Qi J Xie Y Zhang X Hu S Xu Y Lu Y Wu W Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats
description	Xiaoyang Li, Jianping Qi, Yunchang Xie, Xi Zhang, Shunwen Hu, Ying Xu, Yi Lu, Wei WuKey Laboratory of Smart Drug Delivery of Ministry of Education and People&#39;s Liberation Army (PLA), School of Pharmacy, Fudan University, Shanghai, ChinaAbstract: This study aimed to prepare nanoemulsions coated with alginate/chitosan for oral insulin delivery. Uncoated nanoemulsions were prepared by homogenization of a water in oil in water (w/o/w) multiple emulsion that was composed of Labrafac&reg; CC, phospholipid, Span&trade; 80 and Cremorphor&reg; EL. Coating of the nanoemulsions was achieved based on polyelectrolyte cross-linking, with sequential addition of calcium chloride and chitosan to the bulk nanoemulsion dispersion that contained alginate. The particle size of the coated nanoemulsions was about 488 nm and the insulin entrapment ratio was 47.3%. Circular dichroism spectroscopy proved conformational stability of insulin against the preparative stress. In vitro leakage study indicated well-preserved integrity of the nanoemulsions in simulated gastric juices. Hypoglycemic effects were observed in both normal and diabetic rats. The relative pharmacological bioavailability of the coated nanoemulsion with 25 and 50 IU/kg insulin were 8.42% and 5.72% in normal rats and 8.19% and 7.84% in diabetic rats, respectively. Moreover, there were significantly prolonged hypoglycemic effects after oral administration of the coated nanoemulsions compared with subcutaneous (sc) insulin. In conclusion, the nanoemulsion coated with alginate/chitosan was a potential delivery system for oral delivery of polypeptides and proteins.Keywords: insulin, oral delivery, alginate, chitosan, nanoemulsion
format	article
author	Li X Qi J Xie Y Zhang X Hu S Xu Y Lu Y Wu W
author_facet	Li X Qi J Xie Y Zhang X Hu S Xu Y Lu Y Wu W
author_sort	Li X
title	Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats
title_short	Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats
title_full	Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats
title_fullStr	Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats
title_full_unstemmed	Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats
title_sort	nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/f030047e68354f13a5c1d4dd1ac9f685
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Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats

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