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山东大学学报(医学版) ›› 2017, Vol. 55 ›› Issue (8): 42-47.doi: 10.6040/j.issn.1671-7554.0.2017.339

• 基础医学 • 上一篇    下一篇

PEG包衣左氧氟沙星脂质体的制备及性质

张新科1,陈英2,李鹏3,陈洪元4,黄桂华5   

  1. 1.山东大学药学院新药筛选平台, 山东 济南 250012;2.日照市人民医院妇产科, 山东 日照 276826;3.山东省环境保护科学研究设计院, 山东 济南 250013;4.山东大学附属省立医院普外科, 山东 济南 250021;5.山东大学药学院药物制剂研究所, 山东 济南 250012
  • 收稿日期:2017-04-19 出版日期:2017-08-10 发布日期:2017-08-10
  • 通讯作者: 黄桂华. E-mail:hghyj@sdu.edu.cn E-mail:hghyj@sdu.edu.cn

Preparation and characterization of PEG coating levofloxacin-liposomes

ZHANG Xinke1, CHEN Ying2, LI Peng3, CHEN Hongyuan4, HUANG Guihua5   

  1. 1. Drug Screening Platform, School of Pharmaceutical Science, Shandong University, Jinan 250012, Shandong, China;
    2. Department of Gynaecology and Obstetrics, Rizhao Municipal Peoples Hospital, Rizhao 276826, Shandong, China;
    3. Shandong Academy of Environmental Science, Jinan 250013, Shandong, China;
    4. Department of General Surgery, Shandong Provincial Hospital Affiliated to Shandong University, Jinan 250021, Shandong, China;
    5.Institute of Pharmaceutics, School of Pharmaceutical Science, Shandong University, Jinan 250012, Shandong, China
  • Received:2017-04-19 Online:2017-08-10 Published:2017-08-10

摘要: 目的 制备PEG2000包衣左氧氟沙星脂质体,并对其理化性质、初步稳定性及动力学特性进行评价。 方法 选用硫酸铵梯度法制备左氧氟沙星脂质体,以包封率及稳定性为指标筛选PEG2000包衣左氧氟沙星脂质体的最佳制备工艺;采用透射显微镜观察脂质体的外观形态;电位激光粒度分析仪测定粒径及表面Zeta电位;动态膜透析法测定脂质体体外释药特性;对其初步稳定性进行考察;对其体内药动学进行研究。 结果 PEG2000包衣左氧氟沙星脂质体形态圆整,粒径分布均匀,包封率为(77.97±1.09)%,稳定性及体内外缓释性能均好于未包衣左氧氟沙星脂质体。 结论 构建的PEG包衣左氧氟沙星脂质体能明显改善脂质体的稳定性,能为提高脂质体的贮存稳定性开辟一条新途径。

关键词: 硫酸铵梯度法, PEG包衣, 肺靶向脂质体, 稳定性, 左氧氟沙星

Abstract: Objective PEG2000 was used to coat levofloxacin-liposomes(Lvf-lips)in order to improve the stability. The physico-chemical property, preliminary stability and pharmacokinetics of PEG 2000 coating levofloxacin-liposome(PEG Lvf-lips)were systematically investigated. Methods Lvf-lips were prepared by ammonium sulfate gradients method, and the optimal preparation technique of PEG Lvf-lips was screened based on the entrapment efficiency and preliminary stability. The properties of PEG Lvf-lips, such as morphology, diameter and size distribution, were observed with transmission electric microscope, laser dispersive analyzing and micro-electrophoresis apparatus. In vitro drug release of PEG Lvf-lips was performed with the dialysis bag diffusion technique. The pharmacokinetics property was also studied. Results PEG Lvf-lips had spherical shapes and uniform particle size. The entrapment efficiency was(77.97±1.09)%. The stability and sustained release effects in vitro and in vivo PEG Lvf-lips were superior to non-PEG coating liposomes. Conclusion PEG 2000 coating can significantly improve the stability of Lvf-lips, which provides a new pathway for liposome stability.

Key words: Levofloxacin, Pulmonary targeted liposome, Ammonium sulfate gradients method, PEG coating, Stability

中图分类号: 

  • R944.9
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