大黄酚pH敏感性脂质体的制备及其质量评价  

Preparation and quality evaluation of pH-sensitive chrysophanol liposomes

作　　者：庚丽丽[1] 隋琳[2] 张朋美[1] 卢国胜[1] 赵子兵[3] 王永利[1] 

机构地区：[1]河北北方学院应用化学研究所,张家口075000 [2]内蒙古医科大学,呼和浩特010100 [3]太原理工大学,太原030000

出　　处：《中国新药杂志》2017年第10期1189-1193,共5页Chinese Journal of New Drugs

基　　金：河北省科技厅课题(12276104D-94);河北省教育厅课题(QN2015221);河北省卫生厅课题(20160028)

摘　　要：目的:建立大黄酚pH敏感性脂质体的制备工艺并对其进行质量考察。方法:采用薄膜-超声分散法制备大黄酚脂质体,并用羧甲基壳聚糖修饰制得大黄酚pH敏感型脂质体,并对制剂进行包封率、形态学、粒径分布、Zeta电位、稳定性等性质进行考察。结果:本研究制备的大黄酚pH敏感性脂质体的水化介质为Tris缓冲溶液,羧甲基壳聚糖浓度为0.2%(w/v),采用外加溶液方式加入,修饰时间为30 min,制得的大黄酚pH敏感型脂质体稳定性好,pH敏感性好,包封率达(83.73±1.57)%,粒径(494.6±9.6)nm,Zeta电位(-47.60±1.08)m V。结论:采用羧甲基壳聚糖修饰的大黄酚pH敏感性脂质体具有较高的包封率,稳定性好,粒径分布均匀。Objective： To study the preparation method and quality evaluation of pH-sensitive chrysophanol liposomes. Methods： The pH-sensitive liposomes modified with CMCS were prepared by film-ultrasonic dispersion method, then the entrapment efficiency, SEM, particle size distribution, Zeta potential and stability were studied. Results ： The optimal formulation was as follows ： the hydration medium was Tris buffer, the concentration of CMCS was 0.2% （W/V） , the adding method was external addition, and the modification time was 30 min. Under this condition, the entrapment efficiency was （83.73 ± 1.57）% , the uniform particle size was （494.6 ±9.6） nm, and the zeta potential was（ -47.60 ± 1.08） mV. Conclusion： The pH-sensitive liposomes with CMCS modification prepared by film-ultrasonic dispersion method have relatively high entrapment efficiency, with good stability and uniform size distribution, and are sensitive to pH value.

关 键 词：羧甲基壳聚糖 大黄酚 pH敏感性脂质体 包封率 

分 类 号：R944[医药卫生—药剂学]