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Two Novel Freeze-Dried pH-Sensitive Cyclosporine A Nanoparticles: Preparation, in vitro Drug Release, and in vivo Absorption Enhancement Effects
Fang Zhi-gang1; Pan Ping1; Yang Zhi-qiang1; Chen Ya-gen1; Zhang Jian-kang1; Wei Miao1; Zhang Xue-nong1; Zhang Qiang2
关键词Nanoparticle cyclosporine A freeze-drying enhancement absorption pharmacokinetics bioavailability
刊名CURRENT NANOSCIENCE
2009-11-01
5期:4页:449-456
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biotechnology & Applied Microbiology ; Nanoscience & Nanotechnology ; Materials Science, Multidisciplinary
研究领域[WOS]Biotechnology & Applied Microbiology ; Science & Technology - Other Topics ; Materials Science
关键词[WOS]ORAL DELIVERY ; INTRAINDIVIDUAL VARIABILITY ; POLYMERIC NANOPARTICLES ; PLGA NANOPARTICLES ; PARTICLE-SIZE ; DOSAGE FORMS ; PHARMACOKINETICS ; FORMULATION ; ACID ; RATS
英文摘要

The present study was aimed at preparation and performance evaluation of pH-sensitive cyclosporine A (CyA) nanoparticles (CyA-NPs) to improve the poor bioavailability of lipophilic CyA. CyA-NPs were prepared with two types of Eudragit (R) copolymers (Eudragit (R) S100 and Eudragit (R) L100) by a quasi-emulsion solvent diffusion technique. Freeze-dried formulations (Lac-CyA-S100-NP and Lac-CyA-L100-NP) were also prepared. The physical properties, particle size, encapsulation efficiency, and in vitro drug release characteristics were studied. The in vivo bioavailability of CyA-NP and Lac-CyA-S100-NP was investigated in rats at a dose of 15 mg/kg and compared with that of the commercial formulation, Sandimmune Neoral (R). The mean particle size of the CyA-NPs was less than 50 nm, and the encapsulation efficiency was over 99%. Characteristics of the freeze-dried nanoparticles were found to remain relatively stable when lactose was used as a cryoprotectant. In vitro release studies revealed that the CyA-NPs exhibited significant pH-sensitivity. The relative bioavailabilities of CyA-L100-NP, CyA-S100-NP, and Lac-CyA-S100-NP were 117.3%, 162.1%, and 130.1%, respectively, when compared with that of Neoral (R). Therefore, CyA-NPs were considered to be promising oral delivery systems for enhancement of the absorption of the poorly soluble drug, CyA. Freeze-dried nanoparticles could be developed into a novel and effective CyA formulations.

语种英语
WOS记录号WOS:000271386500007
项目编号2006BAI09B00 ; 07C26223201333 ; BS2005022 ; JHB05-46 ; H200630
资助机构National Key Technology RD Program ; National Science and Technology Ministry ; Social Development Foundation of Jiangsu Province ; department of Education of Jinagsu Province ; health department of Jinagsu Province
引用统计
被引频次:5[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/400002259/58299
专题北京大学药学院_药剂学系
作者单位1.Soochow Univ, Coll Pharm, Suzhou 215123, Jiang Su, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Fang Zhi-gang,Pan Ping,Yang Zhi-qiang,et al. Two Novel Freeze-Dried pH-Sensitive Cyclosporine A Nanoparticles: Preparation, in vitro Drug Release, and in vivo Absorption Enhancement Effects[J]. CURRENT NANOSCIENCE,2009,5(4):449-456.
APA Fang Zhi-gang.,Pan Ping.,Yang Zhi-qiang.,Chen Ya-gen.,Zhang Jian-kang.,...&Zhang Qiang.(2009).Two Novel Freeze-Dried pH-Sensitive Cyclosporine A Nanoparticles: Preparation, in vitro Drug Release, and in vivo Absorption Enhancement Effects.CURRENT NANOSCIENCE,5(4),449-456.
MLA Fang Zhi-gang,et al."Two Novel Freeze-Dried pH-Sensitive Cyclosporine A Nanoparticles: Preparation, in vitro Drug Release, and in vivo Absorption Enhancement Effects".CURRENT NANOSCIENCE 5.4(2009):449-456.
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