Comparative study of Pluronic (R) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats

doi:10.1016/j.ijpharm.2013.04.002

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	Comparative study of Pluronic (R) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats
	Chen, Dan; Xia, Dengning; Li, Xiuying; Zhu, Quanlei; Yu, Hongzhen; Zhu, Chunliu; Gan, Yong
刊名	INTERNATIONAL JOURNAL OF PHARMACEUTICS
	2013-06-05
卷号	449 期号:1-2 页码:1-9
关键词	Mucus penetration Oral absorption Pluronic (R) F127 Chitosan Liposomes Cyclosporine A
ISSN号	0378-5173
DOI	10.1016/j.ijpharm.2013.04.002
文献子类	Article
英文摘要	Liposomes modified using cationic and hydrophilic nonionic polymers are 2 popular carriers for improving oral drug absorption. Cationic polymer-modified liposomes can adhere to the intestinal wall mucus (mucoadhesive type), while liposomes modified using hydrophilic nonionic polymers can penetrate across the mucus barrier (mucus-penetrating type). Chitosan-modified liposomes (CS-Lip, mucoadhesive type) and Pluronic (R) F127-modified liposomes (PF127-Lip, mucus-penetrating type) were engineered to investigate the differences between these mucoadhesive and mucus-penetrating systems in oral absorption of a poorly soluble drug, cyclosporine A (CyA). Stability of CS-Lip and PF127-Lip was studied in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The intestinal mucus adhesion or penetration of liposomes was studied by confocal laser scanning microcopy and fluorophotometry using coumarin 6 as the fluorescent probe. The oral absorption of CyA-loaded liposomes was also studied in Sprague-Dawley rats. In vitro and in vivo studies revealed that CS-Lip tended to aggregate in SIF, to be trapped by mucus, to remain mainly in the upper portion of the intestinal tract, and to show limited penetration ability. In contrast, PF127-Lip were more stable in the SIF and SGF, were found throughout the intestinal tract, and were able to penetrate the mucus layers to reach the epithelial surface. Pharmacokinetic analysis in rats showed that the C-max and AUC(0-t) of PF127-Lip were 1.73- and 1.84-fold higher than those of CS-Lip, respectively (P < 0.05). In conclusion, the stability and mucus-penetrating ability of PF127-Lip in the gastrointestinal tract rendered it more suitable than the mucoadhesive CS-Lip for oral delivery CyA. (C) 2013 Elsevier B. V. All rights reserved.
资助项目	National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2012ZX09301001-001] ; Novo Nordisk-Chinese Academy of Science Research Foundation[NNCAS-2009-10] ; National Natural Science Foundation of China[81202468] ; National Basic Research Program of China[2009CB930300] ; SA-SIBS Scholarship Program[00000000]
WOS关键词	DRUG-DELIVERY-SYSTEM ; GASTROINTESTINAL MUCUS ; COATED LIPOSOMES ; IN-VITRO ; POLYMERIC NANOPARTICLES ; INTESTINAL-ABSORPTION ; LIPID-MEMBRANES ; TRITON X-100 ; BIOAVAILABILITY ; PARTICLES
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000319052800001
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277589]
专题	药物制剂研究中心
通讯作者	Gan, Yong
作者单位	Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Chen, Dan,Xia, Dengning,Li, Xiuying,et al. Comparative study of Pluronic (R) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2013,449(1-2):1-9.
APA	Chen, Dan.,Xia, Dengning.,Li, Xiuying.,Zhu, Quanlei.,Yu, Hongzhen.,...&Gan, Yong.(2013).Comparative study of Pluronic (R) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats.INTERNATIONAL JOURNAL OF PHARMACEUTICS,449(1-2),1-9.
MLA	Chen, Dan,et al."Comparative study of Pluronic (R) F127-modified liposomes and chitosan-modified liposomes for mucus penetration and oral absorption of cyclosporine A in rats".INTERNATIONAL JOURNAL OF PHARMACEUTICS 449.1-2(2013):1-9.