In vitro and in vivo evaluation of chitosan graft glyceryl monooleate as peroral delivery carrier of enoxaparin

doi:10.1016/j.ijpharm.2014.05.050

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	In vitro and in vivo evaluation of chitosan graft glyceryl monooleate as peroral delivery carrier of enoxaparin
	Wang, Linlin 2; Li, Liang2 ; Sun, Yujiao 2; Ding, Jiaojiao 2; Li, Jinfeng 2; Duan, Xiaopin 2; Li, Yaping1 ; Junyaprasert, Varaporn B.3; Mao, Shirui 2
刊名	INTERNATIONAL JOURNAL OF PHARMACEUTICS
	2014-08-25
卷号	471 期号:1-2 页码:391-399
关键词	Chitosan Glyceryl monooleate Oral Enoxaparin Polyelectrolyte nanocomplexes
ISSN号	0378-5173
DOI	10.1016/j.ijpharm.2014.05.050
文献子类	Article
英文摘要	In this paper a novel copolymer, chitosan graft glyceryl monooleate (CS-GO) was synthesized and its potential as the nanocarrier for enhancing the peroral delivery of enoxaparin was studied systemically. The successful synthesis was characterized by H-1 NMR. Enoxaparin nanocomplexes were prepared by self-assembly. Mucoadhesive properties of the nanocomplexes were evaluated using mucin particle method. Uptake and transport of the nanocomplexes were investigated in Caco-2 cells. In vivo absorption was studied in rats. The therapeutic effects of the nanocomplexes were evaluated using pulmonary thromboembolism model in mice. This study demonstrated that compared to chitosan based system, hydrophobic modification of CS with GO enhanced the oral absorption of enoxaparin significantly, which is in good agreement with the enhanced mucoadhesion, cellular internalization and transport in cell culture. Cellular uptake of CS-GO based enoxaparin nanocomplexes was incubation time, enoxaparin concentration and incubation temperature dependent. The uptake mechanism was assumed to be adsorptive endocytosis via clathrin- and caveolae-mediated process. Its therapeutic efficacy was further demonstrated by pharmacodynamic study with pulmonary thromboembolism inhibition percentage 47.1%. In conclusion, CS-GO copolymer is a promising nanocarrier for enhancing the oral absorption of enoxaparin. (C) 2014 Elsevier B.V. All rights reserved.
资助项目	Natural Science Foundation of China[81273446] ; Sino-Thai Joint Research and Development Project[9-503J] ; Ministry of Science and Technology of the People's Republic of China[00000000]
WOS关键词	ORAL DELIVERY ; GENE DELIVERY ; PHYSICOCHEMICAL PROPERTIES ; DRUG-DELIVERY ; DNA DELIVERY ; NANOPARTICLES ; INSULIN ; ACID ; NANOCOMPLEXES ; TRANSFECTION
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000338423600046
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276937]
专题	药物制剂研究中心
通讯作者	Mao, Shirui
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Pharmaceut, Shanghai 201203, Peoples R China; 2.Shenyang Pharmaceut Univ, Sch Pharm, Shenyang 110016, Peoples R China; 3.Mahidol Univ, Dept Pharm, Fac Pharm, Bangkok 10400, Thailand
推荐引用方式 GB/T 7714	Wang, Linlin,Li, Liang,Sun, Yujiao,et al. In vitro and in vivo evaluation of chitosan graft glyceryl monooleate as peroral delivery carrier of enoxaparin[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2014,471(1-2):391-399.
APA	Wang, Linlin.,Li, Liang.,Sun, Yujiao.,Ding, Jiaojiao.,Li, Jinfeng.,...&Mao, Shirui.(2014).In vitro and in vivo evaluation of chitosan graft glyceryl monooleate as peroral delivery carrier of enoxaparin.INTERNATIONAL JOURNAL OF PHARMACEUTICS,471(1-2),391-399.
MLA	Wang, Linlin,et al."In vitro and in vivo evaluation of chitosan graft glyceryl monooleate as peroral delivery carrier of enoxaparin".INTERNATIONAL JOURNAL OF PHARMACEUTICS 471.1-2(2014):391-399.