辅酶Q10硫辛酸复配脂质体的制备与表征

Preparation and Characterization of Liposome Containing both Coenzyme Q10 and Alpha Lipoic Acid

目的制备一种负载辅酶Q10和硫辛酸的复配脂质体,考察其物理化学性质。方法选择大豆卵磷脂、胆固醇作为油相,聚山梨酯80作为表面活性剂,采用乙醇注入法制备脂质体并通过正交实验优化配方。结果按照优化方案制备的脂质体辅酶Q10包封率97.03%,硫辛酸包封率88.92%,平均粒径183.4 nm,多分散指数(PDI)小于0.28,Zeta电位-6.9mV,透射电镜下呈球形,粒径大小与光子相关谱(PCS)结果一致。该脂质体具有良好的离心、冻融、静止稳定性,pH与人体皮肤表面pH相似,通过脂质体包裹,辅酶Q10和硫辛酸的稳定性明显提升,且其体外释放速率大大减慢。结论该脂质体制备方法简单,包封率高,粒径较小,具有良好的物理稳定性和应用前景。

Objective To prepare and characterize liposome containing both coenzyme Q10 and alpha lipoic acid （CAL）.Methods CALs were prepared using ethanol injection method with soy phosphatidylcholine （PC） and cholesterol as oil phase and tween-80 as surfactant.The orthogonal design was applied to the optimization of the formulation.Results According to the optimized formulation,the entrapment efficiency of coenzyme Q10 was 97.03 ％ and the entrapment efficiency of alpha lipoic acid was 88.92 ％.The average particle size,PDI and zeta potential were 183.4 nm,0.28 and -6.9 mV,respectively.The shape of CALs was spherical under transmission electron microscope,which was in good coincidence with size study.Furthermore,CALs showed good centrifugation,freezing-thawing and static stability,and the pH of CALs suspension was corresponding to the skin surface condition.Meanwhile,because of the protection of liposome,the stability of coenzyme Q10 and alpha lipoic acid were greatly improved,and CALs displayed a prolonged drug release profile in in vitro release study.Conclusion The preparation process of CALs can be simple with higher entrapment efficiency,smaller particle size and excellent stability,and can have broad potential applications.