蛇床子素脂质体的制备及表征

Preparation and Characterization of Osthole Liposomes

目的:对蛇床子素脂质体的制备方法、制备处方、制剂性质进行研究,并制备冻干脂质体提高制剂的稳定性。方法:以包封率和粒径分布为指标,筛选脂质体的制备方法;采用单因素方差分析和正交实验优化处方,测定优化后处方包封率、粒径、电位,观察电镜下形态;选择甘露醇为冻干保护剂,探究其加入量对冻干脂质体包封率的影响。结果:通过筛选选择乙醇注入法制备脂质体,制备温度为50℃,蛋黄卵磷脂(egg yolk lecithin,EPC)浓度为4mg·mL^-1,胆固醇(cholesterol,CHOL)加入量为5mg,蛇床子素(osthole,Ost)加入量为2mg为最优处方。脂质体包封率为(83.09±0.56)%,粒径为(101.9±2.7)nm,电位(-15.3±2.3)mV。当甘露醇加入量为8%时,冻干脂质体形态较好、复溶后泄漏较少。结论:使用乙醇注入法制备得到的脂质体包封率高,粒径分布均匀,方法稳定,制备为冻干脂质体后,脂质体稳定性得到提高。

Objective:To research the preparation methods,prescriptions and preparation properties of osthole loaded liposomes,and the lyophilized liposomes was prepared to improve the stability of the preparation.Methods:Encapsulation efficiency was taken as index to screen the preparation of liposomes;the formulation was optimized by single factor prescription analysis and orthogonal test.The encapsulation efficiency,particle size and potential of the osthole liposomes were measured,and the morphology under transmission electron microscope was observed;mannitol was selected as a freeze-drying agent,we explored the effect of its addition on the encapsulation efficiency of lyophilized liposomes.Results:The liposomes were prepared by ethanol injection method.The optimal formulations were EPC 4 mg·mL^-1,CHOL 5 mg,Ost 2 mg,and at 50℃ reactive temperature.The encapsulation efficiency of liposome was (83.09±0.56)%,the particle size was(101.9±2.7) nm,and the potential was(-15.3±2.3) mV.When the amount of mannitol was 8%,the lyophilized liposomes had better morphology and less leakage.Conclusion:Liposome which has high entrapment efficiency and well-distributed particle size was prepared by ethanol injection.After preparation of lyophilized liposomes,the stability of liposomes was improved.