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学科主题: 药学
题名:
Bioavailability and pharmacokinetics of cyclosporine A-loaded pH-sensitive nanoparticles for oral administration
作者: Wang, XQ; Dai, JD; Chen, Z; Zhang, T; Xia, GM; Nagai, T; Zhang, Q
关键词: cyclosporine A ; pH-sensitive ; nanoparticles ; suspending agents ; oral administration ; bioavailability ; phannacokinetics ; rats
刊名: JOURNAL OF CONTROLLED RELEASE
发表日期: 2004-07-07
DOI: 10.1016/j.jconrel.2004.03.003
卷: 97, 期:3, 页:421-429
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]: Chemistry ; Pharmacology & Pharmacy
关键词[WOS]: PARTICLE-SIZE ; RELEASE RATES ; DOSAGE FORMS ; MICROSPHERES ; POLYCAPROLACTONE ; NANOSPHERES
英文摘要:

The pH-sensitive cyclosporine A (CyA) nanoparticles were prepared by the solvent displacement method with enteric dissolved polymer of hydroxypropyl methylcellulose phthalate (HPMCP; including HP50 and HP55). The CyA nanoparticles were analyzed by HPLC for yield and encapsulation efficiency, dynamic light scattering for particle size and transmission electron microscopy (TEM) for morphology. The bioavailability of CyA-HP50 and CyA-HP55 nanoparticle colloids were evaluated in rats, compared with the current available CyA microemulsion (Neoral(R)). The bioavailability of CyA-HP55 nanoparticle colloids with various suspending agents was also investigated. The results obtained demonstrated that the pH-sensitive CyA nanoparticles with a particle size of 50-60 nm and encapsulation efficiency over 95% could be reproducibly prepared. The bioavailability of CyA-HP50 and CyA-HP55 nanoparticle colloids calculated by the AUC(0-72) were 82.3% and 119.6%, similar to the reference of Neoral, while the bioavailability of CyA-HP55 nanoparticle colloids was found to be higher than that of CyA-HP50 nanoparticle colloids. The increase of mean residence time (MRT) and the decrease of elimination constant of the central compartment (K-10) for both CyA-HP50 and CyA-HP55 nanoparticle colloids compared with the reference indicated significant sustained release of CyA from the nanoparticles. The effects of the suspending agents on the bioavailability of CyA-HP55 nanoparticles were observed, and the bioavailability decreased as the concentration of suspending agents or the viscosity of the nanoparticle colloids increased. (C) 2004 Elsevier B.V. All rights reserved.

语种: 英语
WOS记录号: WOS:000222531500003
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60548
Appears in Collections:北京大学药学院_药剂学系_期刊论文

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作者单位: 1.Hoshi Univ, Dept Pharmaceut, Tokyo 1428501, Japan
2.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100083, Peoples R China
3.New Drugs R&D Ctr, N China Pharmaceut Grp, Shijiazhuang 050015, Peoples R China

Recommended Citation:
Wang, XQ,Dai, JD,Chen, Z,et al. Bioavailability and pharmacokinetics of cyclosporine A-loaded pH-sensitive nanoparticles for oral administration[J]. JOURNAL OF CONTROLLED RELEASE,2004,97(3):421-429.
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