中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes

文献类型:期刊论文

作者Liu, Yan2; Luo, Xiao3; Xu, Xiaochao2; Gao, Nannan1; Liu, Xiaohong2
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
出版日期2017-01-30
卷号517期号:1-2页码:1-7
关键词Oleanolic acid Liposomes Polyvinylpyrrolidone Sodium deoxycholate Bioavailability
ISSN号0378-5173
DOI10.1016/j.ijpharm.2016.11.056
文献子类Article
英文摘要The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and cholesterol lipid bilayer, a protective hydrophilic polyvinylpyrrolidone-K30 (PVP-K30) coating, and a protective bile salt, sodium deoxycholate, were prepared by a thin-film dispersion method coupled with sonication. Several properties of the PVP-modified OA liposomes (PVPOALs), including surface morphology, particle size, zeta potential and entrapment efficiency were extensively characterized. The pharmacokinetic parameters of PVPOALs in rats were determined by UPLC-MS/MS following oral administration. The results of the characterization studies demonstrated that PVPOALs were spherical particles with an average particle size of 179.4 nm and a zeta potential of -28.8 mV. The drug encapsulation efficiency was more than 90%. After freeze-drying, the prepared liposomes possessed high entrapment efficiency of more than 90%. The mean particle size was 194.8 nm, and the zeta potential was about -30.9 mV. Furthermore, as compared to the commercial tablets, the liposomal formulation enhanced the maximum plasma concentration (C-max) of OA by 6.90-fold in rat plasma. The relative bioavailability of PVP-modified liposomes was 607.9%. The research work in the paper suggests that PVP-modified liposomes could serve as a practical oral preparation for OA in future cancer therapy. (C) 2016 Elsevier B.V. All rights reserved.
WOS关键词ENHANCED ORAL BIOAVAILABILITY ; INSULIN-LOADED LIPOSOMES ; DRUG-DELIVERY SYSTEM ; BILE-SALTS ; PHOSPHOLIPID COMPLEX ; SURFACE MODIFICATION ; PEPTIDE DELIVERY ; CYCLOSPORINE-A ; STABILITY ; CHITOSAN
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000392775100001
出版者ELSEVIER SCIENCE BV
源URL[http://119.78.100.183/handle/2S10ELR8/275663]  
专题中国科学院上海药物研究所
通讯作者Liu, Xiaohong
作者单位1.Shenyang Pharmaceut Univ, Sch Tradit Chinese Med, 103 Wenhua Rd, Shenyang 110016, Peoples R China
2.Shenyang Pharmaceut Univ, Sch Pharm, Dept Biopharmaceut, 103 Wenhua Rd, Shenyang 110016, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, 501 Haike Rd, Shanghai 201210, Peoples R China;
推荐引用方式
GB/T 7714
Liu, Yan,Luo, Xiao,Xu, Xiaochao,et al. Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2017,517(1-2):1-7.
APA Liu, Yan,Luo, Xiao,Xu, Xiaochao,Gao, Nannan,&Liu, Xiaohong.(2017).Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes.INTERNATIONAL JOURNAL OF PHARMACEUTICS,517(1-2),1-7.
MLA Liu, Yan,et al."Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes".INTERNATIONAL JOURNAL OF PHARMACEUTICS 517.1-2(2017):1-7.

入库方式: OAI收割

来源:上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。