硫酸铵梯度法结合微滤膜挤出制备马钱子碱脂质体的研究

Preparation of brucine liposome by a combination of ammonium sulfate transmembrane gradients method and extrusion through microfiltration membranes

目的:探讨马钱子碱脂质体的制备工艺。方法:采用硫酸铵梯度法和微滤膜挤出法制备马钱子碱脂质体,以颗粒形态、粒度和包封率为指标优选硫酸铵梯度法的工艺参数。结果:马钱子碱脂质体的最佳制备条件是:大豆卵磷脂与胆固醇之比为100∶15,0.1 mol/L硫酸铵水溶液的用量为大豆卵磷脂的66.7倍(g.mL-1),马钱子碱加入量为大豆卵磷脂的0.0167倍(g/g),温孵温度为40℃,温孵时间为20 m in。在此条件下制得的马钱子碱脂质体包封率在90%以上,载药量0.25 mg.mL-1,载脂量15 mg.mL-1。结论:硫酸铵梯度法结合微滤膜挤出制备马钱子碱脂质体的工艺可行。

AIM： To preparate brucine liposome. METHODS： Brucine liposomes were preparated by a combination of ammonium sulfate transmembrane gradients method and extrusion through microfihration membranes. The methods were evaluated by particle morphology, the size range, and encapsulation efficiency. RESULTS： The optimal preparating process parameters of brucine nanometer liposome were lecithin-to-cholesterin ratio of 100： 15, the volume of 0.1 mol/L of water solution of ammonium sulfate being 66.7 times as large as lecithin, the volume of brucine being 0.0167 times than lecithin, the temperature and the time of incubating being 40 ~C and 20 min, respectively. The encapsulation efficiency of this method was over 90%. CONCLUSION： Preparation of brucine liposomes by a combination of ammonium sulfate transmembrane gradients method and extrusion through microfiltration membranes is feasible.