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	In vitro and in vivo evaluation of a novel oral insulin formulation
	Ma, Er-li ; Ma, Hong ; Liu, Zheng ; Zheng, Chang-xue ; Duan, Ming-xing
	2010-05-11 ; 2010-05-11 ; OCT
关键词	insulin oral delivery Caco-2 diabetic beagles W/O/W MULTIPLE EMULSIONS CACO-2 CELL MONOLAYERS DRUG-DELIVERY SYSTEMS INTESTINAL-ABSORPTION TIGHT JUNCTIONS DIABETIC-RATS TRANSPORT MACROMOLECULES CHROMATOGRAPHY MICROEMULSION Chemistry, Multidisciplinary Pharmacology & Pharmacy
中文摘要	Aim: To develop a stable self-emulsifying formulation for oral delivery of insulin. Methods: Caco-2 cell line and diabetic beagles were used as in vitro and in vivo models to study the absorption mechanism and the hypoglycemic efficacy of the formulation. In addition, various physicochemical parameters of the formulation such as droplet size, insulin encapsulation efficiency and stability were evaluated. Results: This formulation enabled changes in barrier properties of Caco-2 monolayers, as referred by transepithelial electrical resistance (TEER) and apparent permeability coefficients (P-app) of the paracellular marker ranitidine (20-fold greater than control) but not transcellular marker propranolol, suggesting that the opening of tight junctions was involved. In diabetic beagle dogs, the bioavailability of this formulation was up to 15.2% at a dose of 2.5 IU/kg in comparison with the hypoglycemic effect of native insulin (0.5 IU/kg) delivered by subcutaneous injection. Conclusion: This formulation, recently approved by the China State Food and Drug Administration to enter clinical trials, was stable, degradation-protected and absorption-enhanced, and provided a promising formulation for oral insulin delivery.
语种	英语 ; 英语
出版者	BLACKWELL PUBLISHING ; OXFORD ; 9600 GARSINGTON RD, OXFORD OX4 2DQ, OXON, ENGLAND
内容类型	期刊论文
源URL	[http://hdl.handle.net/123456789/26601]
专题	清华大学
推荐引用方式 GB/T 7714	Ma, Er-li,Ma, Hong,Liu, Zheng,et al. In vitro and in vivo evaluation of a novel oral insulin formulation[J],2010, 2010, OCT.
APA	Ma, Er-li,Ma, Hong,Liu, Zheng,Zheng, Chang-xue,&Duan, Ming-xing.(2010).In vitro and in vivo evaluation of a novel oral insulin formulation..
MLA	Ma, Er-li,et al."In vitro and in vivo evaluation of a novel oral insulin formulation".(2010).

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