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Mesoporous Silica Nanoparticles for Increasing the Oral Bioavailability and Permeation of Poorly Water Soluble Drugs
Zhang, Yanzhuo2; Wang, Jiancheng1; Bai, Xiaoyu1; Jiang, Tongying2; Zhang, Qiang1; Wang, Siling2
关键词drug delivery mesoporous nanoparticles cellular uptake permeability bioavailability
刊名MOLECULAR PHARMACEUTICS
2012-03-01
DOI10.1021/mp200287c
9期:3页:505-513
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Medicine, Research & Experimental ; Pharmacology & Pharmacy
研究领域[WOS]Research & Experimental Medicine ; Pharmacology & Pharmacy
关键词[WOS]CONTROLLED-RELEASE ; SOLID DISPERSIONS ; DELIVERY ; CARRIERS ; MICROPARTICLES ; TRANSPORTERS ; TELMISARTAN ; INCLUSION ; MOLECULES ; DISCOVERY
英文摘要

We investigate the effects of spherical mesoporous silica nanoparticles (MSNs) as an oral drug delivery system to improve the oral bioavailability of the model drug telmisartan (TEL) and examine their cellular uptake and cytotoxicity. Further, we explore the mechanisms behind the improved oral absorption of poorly soluble drugs promoted by MSNs. An investigation of intestinal epithelial cellular binding, association and uptake was carried out by laser scanning confocal microscopy, transmission electron microscopy and fluorescence activated cell sorting. The results show that the cellular uptake is highly time-, concentration- and size-dependent. The model drug permeability studies carcinoma (Caco-2) cell lines indicated that MSNs could significantly enhance TEL permeability and reduce rate of drug efflux. After loading TEL into MSNs, its oral bioavailability was compared with that of the marketed product Micardis and TEL-loaded ordered mesoporous silica microparticles (MSMs) in beagle dogs. The relative bioavailability of TEL-loaded MSN formulation and TEL-loaded MSM formulation was 154.4 +/- 28.4% and 129.1 +/- 15.6%, respectively. MSNs offer the potential to achieve enhanced oral bioavailability of poorly soluble drugs via improved drug dissolution rate and enhanced drug permeability.

语种英语
WOS记录号WOS:000301018200016
项目编号2009CB930300 ; 81072605 ; 2009ZX09301-012
资助机构National Basic Research Program of China (973 Program) ; National Science Foundation of China ; Major National Platform for Innovative Pharmaceuticals
引用统计
被引频次:87[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/400002259/59162
专题北京大学药学院
北京大学药学院_药剂学系
作者单位1.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Shenyang Pharmaceut Univ, Sch Pharm, Dept Pharmaceut, Shenyang 110016, Peoples R China
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GB/T 7714
Zhang, Yanzhuo,Wang, Jiancheng,Bai, Xiaoyu,et al. Mesoporous Silica Nanoparticles for Increasing the Oral Bioavailability and Permeation of Poorly Water Soluble Drugs[J]. MOLECULAR PHARMACEUTICS,2012,9(3):505-513.
APA Zhang, Yanzhuo,Wang, Jiancheng,Bai, Xiaoyu,Jiang, Tongying,Zhang, Qiang,&Wang, Siling.(2012).Mesoporous Silica Nanoparticles for Increasing the Oral Bioavailability and Permeation of Poorly Water Soluble Drugs.MOLECULAR PHARMACEUTICS,9(3),505-513.
MLA Zhang, Yanzhuo,et al."Mesoporous Silica Nanoparticles for Increasing the Oral Bioavailability and Permeation of Poorly Water Soluble Drugs".MOLECULAR PHARMACEUTICS 9.3(2012):505-513.
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