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In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery
Wang, Yancai1; Zhang, Dianrui1; Liu, Zhaoping2; Liu, Guangpu1; Duan, Cunxian1; Jia, Lejiao1; Feng, Feifei1; Zhang, Xiaoyu2; Shi, Yanqiu2; Zhang, Qiang3
刊名NANOTECHNOLOGY
2010-04-16
DOI10.1088/0957-4484/21/15/155104
21期:15
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Nanoscience & Nanotechnology ; Materials Science, Multidisciplinary ; Physics, Applied
研究领域[WOS]Science & Technology - Other Topics ; Materials Science ; Physics
关键词[WOS]DISSOLUTION RATE ENHANCEMENT ; HIGH-PRESSURE HOMOGENIZATION ; POORLY SOLUBLE DRUGS ; LIPID NANOPARTICLES ; CELLULAR UPTAKE ; CACO-2 CELLS ; NANOCRYSTALS ; FORMULATION ; SOLUBILITY ; TECHNOLOGY
英文摘要

In this study, we evaluate the effect of particle sizes on the physicochemical properties of silybin and identify the influence of silybin nanosuspensions on its permeation across the Caco-2 cell monolayer. In vivo pharmacokinetic evaluation of silybin nanosuspensions was also carried out in beagle dogs. TEM, AFM and SEM analyses revealed the effect of homogenization pressure on particle size and morphology, and confirmed the existence of a surfactant-stabilizer film on the surface of nanoparticles. DSC and XRPD experiments manifested that the crystalline state was maintained as particle size was reduced and the enhanced dissolution property was due to the increased surface area. Nanosuspensions had a significant influence on drug transport across the Caco-2 cell monolayer and the enhanced dissolution velocity was responsible for the increased permeability. A pharmacokinetics study in beagle dogs further confirmed the in vitro results and demonstrated that oral administration of silybin nanosuspensions significantly increase its bioavailability compared to the coarse powder. Nanosuspensions of silybin with smaller particle size reveal a higher potential to increase their oral bioavailability; while for intravenous infusion the lower pressure produced silybin nanosuspensions appeared to maintain a more sustained drug release profile.

语种英语
WOS记录号WOS:000275901500004
项目编号2009CB930300
资助机构National Basic Research Program of China (973Program)
引用统计
被引频次:51[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/64835
专题北京大学药学院
作者单位1.Shandong Univ, Dept Pharmaceut, Coll Pharm, Jinan 250012, Peoples R China
2.Shandong Univ, Ctr New Drugs Evaluat, Jinan 250012, Peoples R China
3.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Wang, Yancai,Zhang, Dianrui,Liu, Zhaoping,et al. In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery[J]. NANOTECHNOLOGY,2010,21(15).
APA Wang, Yancai.,Zhang, Dianrui.,Liu, Zhaoping.,Liu, Guangpu.,Duan, Cunxian.,...&Zhang, Qiang.(2010).In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery.NANOTECHNOLOGY,21(15).
MLA Wang, Yancai,et al."In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery".NANOTECHNOLOGY 21.15(2010).
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