PEG包衣左氧氟沙星脂质体的制备及性质  

Preparation and characterization of PEG coating levofloxacin-liposomes

作　　者：张新科[1] 陈英[2] 李鹏[3] 陈洪元[4] 黄桂华[5] 

机构地区：[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

出　　处：《山东大学学报（医学版）》2017年第8期42-47,共6页Journal of Shandong University:Health Sciences

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。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 nonPEG coating liposomes. Conclusion PEG 2000 coating can significantly improve the stability of Lvf-lips,which provides a new pathw ay for liposome stability.

关 键 词：左氧氟沙星 肺靶向脂质体 稳定性 PEG包衣 硫酸铵梯度法 

分 类 号：R944.9[医药卫生—药剂学]