大黄酚pH敏感性脂质体的制备及其质量评价

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缓中溶液,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)mV.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.