Directed Self-assembled Nanoparticles of Probucol Improve Oral Delivery: Fabrication, Performance and Correlation

doi:10.1007/s11095-014-1321-7

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物制剂研究中心

	Directed Self-assembled Nanoparticles of Probucol Improve Oral Delivery: Fabrication, Performance and Correlation
	Zhang, Zhiwen1 ; Jiang, Shijun 2; Liu, Zeying 2; Niu, Baohua 1; Gu, Wangwen1 ; Li, Yaping1 ; Cui, Jingbin 2
刊名	PHARMACEUTICAL RESEARCH
	2014-09
卷号	31 期号:9 页码:2266-2275
关键词	correlation directed self-assembly nanoparticles oral delivery probucol
ISSN号	0724-8741
DOI	10.1007/s11095-014-1321-7
文献子类	Article
英文摘要	We are reporting on the development of a unique drug delivery platform by directed self-assembly technique to improve the oral delivery of hydrophobic drugs. Herein, a series of probucol directed self-assembled nanoparticles (PDN) were developed with two components of probucol and surfactant such as Tween 20, Tween 80, D-alpha-tocopheryl polyethylene glycol 1,000 succinate (TPGS) and HS-15, which was respectively named as T-20-PDN, T-80-PDN, TP-PDN and HS-PDN. The formation of various PDNs was determined by in vitro characterization and the physicochemical properties of these PDNs were determined. Moreover, the performance of PDN in enhancing the oral delivery and possible correlation between the in vitro properties and in vivo performances were investigated. PDN was homogenous nanometer-sized particles with negative surface charge. The cellular uptake of probucol in Caco-2 cell monolayer was respectively increased 1.15, 1.82, 1.59 and 5.31-fold by these PDN. In particular, the oral bioavailability of these PDN was significantly improved 3.0, 4.1, 5.4 and 10.4 folds compared with the free drug suspension. The enhanced cellular uptake and oral bioavailability were correlated with the characters of involved surfactants and the particle size of PDN. Thereby, the directed self-assembled nanoparticles could provide a new strategy for enhancing the oral delivery of hydrophobic drugs.
资助项目	The National Basic Research Program of China[2013CB932503] ; The National Basic Research Program of China[2013CB932704] ; National Natural Science Foundation of China[81270047] ; National Natural Science Foundation of China[81373359] ; SA-SIBS Scholarship Program[00000000]
WOS关键词	LIPID-BASED FORMULATIONS ; IN-VITRO CHARACTERISTICS ; WATER-SOLUBLE DRUGS ; POLYMERIC NANOPARTICLES ; LIPOPHILIC DRUGS ; ABSORPTION ; SYSTEM ; BIOAVAILABILITY ; MECHANISM ; RATS
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	SPRINGER/PLENUM PUBLISHERS
WOS记录号	WOS:000343133900003
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276915]
专题	药物制剂研究中心
通讯作者	Li, Yaping
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Pharmaceut, Shanghai 201203, Peoples R China; 2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Zhiwen,Jiang, Shijun,Liu, Zeying,et al. Directed Self-assembled Nanoparticles of Probucol Improve Oral Delivery: Fabrication, Performance and Correlation[J]. PHARMACEUTICAL RESEARCH,2014,31(9):2266-2275.
APA	Zhang, Zhiwen.,Jiang, Shijun.,Liu, Zeying.,Niu, Baohua.,Gu, Wangwen.,...&Cui, Jingbin.(2014).Directed Self-assembled Nanoparticles of Probucol Improve Oral Delivery: Fabrication, Performance and Correlation.PHARMACEUTICAL RESEARCH,31(9),2266-2275.
MLA	Zhang, Zhiwen,et al."Directed Self-assembled Nanoparticles of Probucol Improve Oral Delivery: Fabrication, Performance and Correlation".PHARMACEUTICAL RESEARCH 31.9(2014):2266-2275.