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首页> 外文期刊>International Journal of Pharmaceutics >Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes
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Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes

机译：PVP改性烯醇酸脂质体的制备，表征和体内药代动力学研究

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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.
机译：本研究的主要目的是设计和优化水溶性药物含油酸（OA）的脂质体制剂，以改善其口腔生物利用度，延长治疗药物水平的持续时间。通过薄膜分散方法与超声处理制备含有大豆卵磷脂和胆固醇脂双层，保护亲水聚乙烯吡咯烷酮-K30（PVP-K30）涂层和保护胆汁盐，脱氧胆酸钠，脂质体。 PVP改性的OA脂质体（PVPOALS）的几种性质，包括表面形态，粒度，ζ电位和熵效率。通过口服给药后UPLC-MS / MS测定大鼠中PVPOALS的药代动力学参数。表征研究的结果表明，PVPoAls是球形颗粒，平均粒径为179.4nm，Zeta电位为-28.8 mV。药物包封效率超过90％。冷冻干燥后，制备的脂质体具有高于90％以上的夹带效率。平均粒径为194.8nm，ζ电位约为-30.9 mV。此外，与商业片剂相比，脂质体制剂在大鼠等离子体中提高了OA的最大血浆浓度（C-MAX）。 PVP改性脂质体的相对生物利用度为607.9％。本文的研究工作表明，PVP改性脂质体可以作为未来癌症治疗中OA的实际口服制剂。 （c）2016 Elsevier B.v.保留所有权利。

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