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
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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 |
DOI | 10.1016/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
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