丹酚酸B脂质体的制备及其体外释药的研究

目的研究丹酚酸B脂质体的制备方法及其体外释放情况。方法采用逆向蒸发法制备丹酚酸B脂质体,超滤离心法测其包封率,以包封率和粒径为指标,采用正交试验设计法优化处方,并对其表面特征、包封率、粒径、体外释放情况进行考察。结果制备的丹酚酸B脂质的体平均粒径为109.8 nm,药物的平均包封率为71.0%,体外12 h累积释放率为43.7%。脂质体外观圆整而均匀,分散性好。结论制备的丹酚酸B脂质体包封率较高,粒径小,有良好的缓释作用,为后期研究其长循环心靶向脂质体奠定了基础。

Preparation of salvianolic acid B liposome and its in vitro release

Objective To study the preparation of salvianolic acid B liposome and its in vitro release. Methods Reverse-phase evaporation technique was chosen for preparation salvianolic acid B liposome and entrapment efficiency was measured by ultrafiltration. Orthogonal design was used to optimize the formulation,by taking encapsulation efficiency and the particle size as indexes. The properties of liposomes including morphology, entrapment efficiency, mean diameter, and accumulative release were studied. Results Mean diameter and encapsulation efficiency of prepared salvianolic acid B liposome were 109.8 nm and 71.0%, respectively. The in vitro 12 h accumulative release was, 43.7% of the total drug. The liposome was smooth and spherieal in appearance with better dispersion. Conclusion The salvianolic acid B liposome prepared in this study have the smaller size and the higher encapsulation efficiency, and the in vitro release could be in a well sustained way, which could provide a basis on the study of long circulating heart-targeted liposome.