Self-assembled liquid crystalline nanoparticles as a novel ophthalmic delivery system for dexamethasone: Improving preocular retention and ocular bioavailability

doi:10.1016/j.ijpharm.2010.06.015

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	Self-assembled liquid crystalline nanoparticles as a novel ophthalmic delivery system for dexamethasone: Improving preocular retention and ocular bioavailability
	Gan, Li 1; Han, Shun 1; Shen, Jinqiu 2; Zhu, Jiabi 2; Zhu, Chunliu1 ; Zhang, Xinxin1 ; Gan, Yong1
刊名	INTERNATIONAL JOURNAL OF PHARMACEUTICS
	2010-08-30
卷号	396 期号:1-2 页码:179-187
关键词	Cubosome Dexamethasone Ocular bioavailability Ophthalmic delivery Preocular retention
ISSN号	0378-5173
DOI	10.1016/j.ijpharm.2010.06.015
文献子类	Article
英文摘要	The object of this study was to design novel self-assembled liquid crystalline nanoparticles (cubosomes) as an ophthalmic delivery system for dexamethasone (DEX) to improve its preocular retention and ocular bioavailability DEX cubosome particles were produced by fragmenting a cubic crystalline phase of monoolein and water in the presence of stabilizer Poloxamer 407. Small angle X-ray diffraction (SAXR) profiles revealed its internal structure as Pn3m space group, indicating the diamond cubic phase. In vitro, the apparent permeability coefficient of DEX administered in cubosomes exhibited a 4.5-fold (F1) and 3 5-fold (F2) increase compared to that of Dex-Na phosphate eye drops Preocular retention studies revealed that the retention of cubosomes was significantly longer than that of solution and carbopol gel, with AUC(0 -> 180min) of Rh B cubosomes being 2-3-fold higher than that of the other two formulations In vivo pharmacokinetics in aqueous humor was evaluated by microdialysis, which indicated a 1 8-fold (F1) increase in AUC(0 -> 240min) of DEX administered in cubosomes relative to that of Dex-Na phosphate eye drops, with about an 8-fold increase compared to that of DEX suspension Corneal cross-sections after incubation with DEX cubosomes demonstrated an unaffected corneal structure and tissue integrity, which indicated the good biocompatibility of DEX cubosomes In conclusion, self-assembled liquid crystalline nanoparticles might represent a promising vehicle for effective ocular drug delivery Crown Copyright (C) 2010 Published by Elsevier B V. All rights reserved
资助项目	National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09301-001] ; National Basic Research Program of China[2009CB930300] ; National High Technology Research and Development Program of China (863 Program)[2007AA021604]
WOS关键词	ALBINO RABBIT CORNEA ; DRUG-DELIVERY ; IN-VITRO ; CUBIC PHASE ; GLYCERYL MONOOLEATE ; BUCCAL PERMEATION ; TOPICAL DELIVERY ; LIPID EMULSION ; ESTER PRODRUGS ; CYCLOSPORINE-A
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000280936000025
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278796]
专题	药物制剂研究中心
通讯作者	Gan, Yong
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China
推荐引用方式 GB/T 7714	Gan, Li,Han, Shun,Shen, Jinqiu,et al. Self-assembled liquid crystalline nanoparticles as a novel ophthalmic delivery system for dexamethasone: Improving preocular retention and ocular bioavailability[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2010,396(1-2):179-187.
APA	Gan, Li.,Han, Shun.,Shen, Jinqiu.,Zhu, Jiabi.,Zhu, Chunliu.,...&Gan, Yong.(2010).Self-assembled liquid crystalline nanoparticles as a novel ophthalmic delivery system for dexamethasone: Improving preocular retention and ocular bioavailability.INTERNATIONAL JOURNAL OF PHARMACEUTICS,396(1-2),179-187.
MLA	Gan, Li,et al."Self-assembled liquid crystalline nanoparticles as a novel ophthalmic delivery system for dexamethasone: Improving preocular retention and ocular bioavailability".INTERNATIONAL JOURNAL OF PHARMACEUTICS 396.1-2(2010):179-187.