胆酸-黄芩苷脂质体的制备

Preparation of cholic acid-baicalin liposomes

目的制备胆酸-黄芩苷脂质体。方法逆向蒸发法制备脂质体。在单因素试验基础上,以胆酸用量、磷脂-药物比例、磷脂-胆固醇比例为影响因素,包封率、载药量为评价指标,Box-Behnken设计优化制备工艺。然后,对所得脂质体进行质量评价,测定其体外释放度。结果最佳条件为胆酸用量9.06 mg,磷脂-药物比例7.23∶1,磷脂-胆固醇比例4.55∶1,包封率44.1%,载药量5.05%。所得脂质体为淡黄色球形或类球形,物理稳定性良好,平均粒径142 nm,PDI 0.190,Zeta电位-7.82 mV,6 h内累积释放率为57.83%,体外释放行为符合双相动力学模型。结论该方法稳定可靠,可用于制备具有缓释作用的胆酸-黄芩苷脂质体。

AIM To prepare cholic acid-baicalin liposomes. METHODS For the liposomes prepared by reverse-phase evaporation method, the preparation technology was optimized by Box-Behnken design on the basis of single factor test, with cholic acid consumption, phospholipid-drug ratio and phospholipid-cholesterol ratio as influencing factors, encapsulation efficiency and drug loading as evaluation indices. Subsequently, the obtained liposomes had their quality evaluated and their in vitro release rate assessed. RESULTS The optimal conditions were determined to be 9.06 mg for cholic acid consumption, 7.23 ∶ 1 for phospholipid-drug ratio, and 4.55 ∶ 1 for phospholipid-cholesterol ratio, the encapsulation efficiency and drug loading were 44.1% and 5.05%, respectively. The obtained light yellow, spherical or spherical-like liposomes demonstrated good physical stability, with the average particle size, PDI, Zeta potential and accumulative release rate within 6 h of 142 nm, 0.190,-7.82 mV and 57.83%, respectively, and the in vitro release behaviors accorded with two-phase kinetic model. CONCLUSION This stable and reliable method can be used for the preparation of cholic acid-baicalin liposomes with sustainedrelease effect.