Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations

Xiong-Bin Hu,1–3 Tian-Tian Tang,1–3 Yong-Jiang Li,1–3 Jun-Yong Wu,1–3 Jie-Min Wang,1–3 Xin-Yi Liu,1–3 Da-Xiong Xiang1–31Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, Hunan, 410011, People...

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Autores principales:	Hu XB, Tang TT, Li YJ, Wu JY, Wang JM, Liu XY, Xiang DX
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	insulin phospholipid complex oral drug delivery nanoemulsion hypoglycemic effect Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/35122b4b66d44f47b7d7bb499ae7746c
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spelling	oai:doaj.org-article:35122b4b66d44f47b7d7bb499ae7746c2021-12-02T07:40:13ZPhospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations1178-2013https://doaj.org/article/35122b4b66d44f47b7d7bb499ae7746c2019-05-01T00:00:00Zhttps://www.dovepress.com/phospholipid-complex-based-nanoemulsion-system-for-oral-insulin-delive-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Xiong-Bin Hu,1–3 Tian-Tian Tang,1–3 Yong-Jiang Li,1–3 Jun-Yong Wu,1–3 Jie-Min Wang,1–3 Xin-Yi Liu,1–3 Da-Xiong Xiang1–31Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, Hunan, 410011, People’s Republic of China; 2Institute of Clinical Pharmacy, Central South University, Changsha 410011, Hunan, People’s Republic of China; 3Hunan Provincial Engineering Research Center of Translational Medicine and Innovative Drug, Changsha, Hunan Province, 410011, People’s Republic of ChinaPurpose: The aim of this research was to develop a phospholipid complex based nanoemulsion system for oral insulin delivery.Methods: Insulin-phospholipid complex (IPC) was firstly prepared by an anhydrous co-solvent lyophilization method, and then encapsulated into the oil phase of nanoemulsion to obtain the IPC-based nanoemulsion (IPC-NE). Both water-in-oil (W/O) IPC-NE and oil-in-water (O/W) IPC-NE were formulated and evaluated for comparison.Results: The obtained W/O IPC-NE and O/W IPC-NE were both spherical in shape with a mean particle size of 18.6±0.79 nm and 27.3±1.25 nm, respectively. While both IPC-NEs exhibited enhanced Caco-2 cell monolayers permeability than IPC and insulin solution, W/O IPC-NE showed relatively greater protective effects against enzymatic degradation than O/W IPC-NE. Moreover, oral administration of W/O IPC-NE exhibited significant hypoglycemic effects, with 12.4-fold and 1.5-fold higher oral bioavailability compared with insulin solution and O/W IPC-NE, respectively.Conclusion: IPC-NEs, especially the W/O IPC-NE showed promising efficiency in vitro and in vivo, thus could be a potential strategy for oral insulin delivery.Keywords: insulin, phospholipid complex, oral drug delivery, nanoemulsion, hypoglycemic effectHu XBTang TTLi YJWu JYWang JMLiu XYXiang DXDove Medical Pressarticleinsulinphospholipid complexoral drug deliverynanoemulsionhypoglycemic effectMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 3055-3067 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	insulin phospholipid complex oral drug delivery nanoemulsion hypoglycemic effect Medicine (General) R5-920
spellingShingle	insulin phospholipid complex oral drug delivery nanoemulsion hypoglycemic effect Medicine (General) R5-920 Hu XB Tang TT Li YJ Wu JY Wang JM Liu XY Xiang DX Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations
description	Xiong-Bin Hu,1–3 Tian-Tian Tang,1–3 Yong-Jiang Li,1–3 Jun-Yong Wu,1–3 Jie-Min Wang,1–3 Xin-Yi Liu,1–3 Da-Xiong Xiang1–31Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, Hunan, 410011, People’s Republic of China; 2Institute of Clinical Pharmacy, Central South University, Changsha 410011, Hunan, People’s Republic of China; 3Hunan Provincial Engineering Research Center of Translational Medicine and Innovative Drug, Changsha, Hunan Province, 410011, People’s Republic of ChinaPurpose: The aim of this research was to develop a phospholipid complex based nanoemulsion system for oral insulin delivery.Methods: Insulin-phospholipid complex (IPC) was firstly prepared by an anhydrous co-solvent lyophilization method, and then encapsulated into the oil phase of nanoemulsion to obtain the IPC-based nanoemulsion (IPC-NE). Both water-in-oil (W/O) IPC-NE and oil-in-water (O/W) IPC-NE were formulated and evaluated for comparison.Results: The obtained W/O IPC-NE and O/W IPC-NE were both spherical in shape with a mean particle size of 18.6±0.79 nm and 27.3±1.25 nm, respectively. While both IPC-NEs exhibited enhanced Caco-2 cell monolayers permeability than IPC and insulin solution, W/O IPC-NE showed relatively greater protective effects against enzymatic degradation than O/W IPC-NE. Moreover, oral administration of W/O IPC-NE exhibited significant hypoglycemic effects, with 12.4-fold and 1.5-fold higher oral bioavailability compared with insulin solution and O/W IPC-NE, respectively.Conclusion: IPC-NEs, especially the W/O IPC-NE showed promising efficiency in vitro and in vivo, thus could be a potential strategy for oral insulin delivery.Keywords: insulin, phospholipid complex, oral drug delivery, nanoemulsion, hypoglycemic effect
format	article
author	Hu XB Tang TT Li YJ Wu JY Wang JM Liu XY Xiang DX
author_facet	Hu XB Tang TT Li YJ Wu JY Wang JM Liu XY Xiang DX
author_sort	Hu XB
title	Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations
title_short	Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations
title_full	Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations
title_fullStr	Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations
title_full_unstemmed	Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations
title_sort	phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/35122b4b66d44f47b7d7bb499ae7746c
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_version_	1718399273742106624

Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations

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