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学科主题: 药学
题名:
Mesoporous Silica Nanoparticles for Increasing the Oral Bioavailability and Permeation of Poorly Water Soluble Drugs
作者: 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
发表日期: 2012-03-01
DOI: 10.1021/mp200287c
卷: 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
所属项目编号: 2009CB930300 ; 81072605 ; 2009ZX09301-012
项目资助者: National Basic Research Program of China (973 Program) ; National Science Foundation of China ; Major National Platform for Innovative Pharmaceuticals
WOS记录号: WOS:000301018200016
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59162
Appears in Collections:北京大学药学院_期刊论文

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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

Recommended Citation:
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.
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