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pH-sensitive nanoparticles for improving the oral bioavailability of cyclosporine A
Dai, JD1; Nagai, T1; Wang, XQ1; Zhang, T1; Meng, M1; Zhang, Q1
关键词Cyclosporine a Ph-sensitive Naroparticles Poly(Methacrylic Acid And Methacrylate) coPolymer Neoral Microemulsion In Vitro Release Oral Bioavailability
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2004-08-06
DOI10.1016/j.ijpharm.2004.05.006
280期:1-2页:229-240
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]DRUG-RELEASE ; POLYCAPROLACTONE NANOPARTICLES ; INTRAINDIVIDUAL VARIABILITY ; MICROSPHERES ; ABSORPTION ; EMULSION ; DELIVERY ; RAT ; GLYCOPROTEIN ; NANOCAPSULES
英文摘要

The purpose of this work was to improve the oral bioavailability of cyclosporine A (CyA) by preparation the CyA-pH sensitive nanoparticles. The CyA-pH sensitive nanoparticles were prepared by using poly(methacrylic acid and methacrylate) copolymer. The characterization and the dispersion state of CyA at the surface or inside the polymeric matrices of the nanoparticles were investigated. The in vitro release studies were conducted by ultracentrifuge method. The bioavailability of CyA from nanoparticles and Neoral microemulsion was assessed in Sprague-Dawley (SD) rats at a dose of 15 mg/kg. The particle size of the nanoparticles was within the range from 37.4 +/- 5.6 to 106.7 +/- 14.8 nm. The drug entrapped efficiency was very high (from 90.9 to 99.9%) and in all cases the drug was amorphous or molecularly dispersed within the nanoparticles polymeric matrices. In vitro release experiments revealed that the nanoparticles exhibited perfect pH-dependant release profiles. The relative bioavailability of CyA was markedly increased by 32.5% for CyA-S100 nanoparticles (P < 0.05), and by 15.2% and 13.6% for CyA-L100-55 and CyA-L100 nanoparticles respectively, while it was decreased by 5.2% from CyA-E100 nanoparticles when compared with the Neoral microemulsion. With these results, the potential of pH-sensitive nanoparticles for the oral delivery of CyA was confirmed. (C) 2004 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000223453200021
引用统计
被引频次:119[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/400002259/50737
专题北京大学药学院_药剂学系
作者单位1.Hoshi Univ, Dept Pharmaceut, Tokyo 1420063, Japan
2.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100083, Peoples R China
3.N China Pharmacet Grp Co Ltd, Inst Pharmaceut, Shijiazhuang, Peoples R China
推荐引用方式
GB/T 7714
Dai, JD,Nagai, T,Wang, XQ,et al. pH-sensitive nanoparticles for improving the oral bioavailability of cyclosporine A[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2004,280(1-2):229-240.
APA Dai, JD,Nagai, T,Wang, XQ,Zhang, T,Meng, M,&Zhang, Q.(2004).pH-sensitive nanoparticles for improving the oral bioavailability of cyclosporine A.INTERNATIONAL JOURNAL OF PHARMACEUTICS,280(1-2),229-240.
MLA Dai, JD,et al."pH-sensitive nanoparticles for improving the oral bioavailability of cyclosporine A".INTERNATIONAL JOURNAL OF PHARMACEUTICS 280.1-2(2004):229-240.
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