二氢杨梅素脂质体的处方优化及性质考察

Study on Optimization and Characterization of Dihydromyricetin Liposome

目的:优化二氢杨梅素脂质体的处方及工艺,并考察其性质。方法:采用薄膜-超声法制备的二氢杨梅素脂质体,以包封率为指标,采用单因素法考察处方及工艺,在此基础上采用正交试验对二氢杨梅素脂质体的处方工艺进行筛选与优化;采用透射电镜观察其形态,采用动态透析法考察其体外释放的特性,并进行初步稳定性研究。结果:二氢杨梅素脂质体最佳处方和工艺条件为:磷脂与胆固醇的摩尔比为1∶1,二氢杨梅素加入量4.0 mg,PBS缓冲液pH为5.0,超声时间3 min。优化后脂质体的包封率为58.1%,电镜下呈球形或近球形小囊泡状,48 h体外累计释放率达到76.29%,4℃下避光放置30天药物含量为加入量的96.57%。结论:二氢杨梅素脂质体处方及制备工艺简单且重复性好,制剂稳定性良好。

This study was aimed to optimize dihydromyricetin liposome formulations by orthogonal design in order to study its characterization. Dihydromyricetin liposomes were prepared with thin-film ultrasonic dispersion technology. Formulations of dihydromyricetin liposomes were optimized with entrapment efficiency as the optimized index. The formulation and technology were evaluated by the single factor. Based on this, orthogonal design was made on the screening and optimization of dihydromyricetin liposome. Its morphology was observed by transmission electron micro-scope. Its in vitro drug-release behavior was studied by equilibrium dialysis. The preliminary stability was studied. The results showed that the optimized formulation and technology of dihydromyricetin liposome was when the molar ratio of lecithin and cholesterol was 1：1, the dosage of dihydromyricetin was 4.0 mg. The pH of PBS was 5.0, ultra-sonic time was 3 min. The encapsulation efficiency of dihydromyricetin liposome was 58.1%. Its morphology was small spherical or nearly spherical vesicle with observation in transmission electron microscope. It showed that the in＆nbsp;vitro release of dihydromyricetin liposome arrived 76.29% in 48 h. The drug content was still 96.57% of dosage for 30 days at 4oC in the dark place. It was concluded that the optimized formulation and preparation technology of di-hydromyricetin liposome were simple, replicable and stable.