肺靶向吡非尼酮脂质体的制备及体外释药性质研究

目的：研究肺靶向吡非尼酮脂质体的制备方法并考察其体外释药性质。方法：采用薄膜分散法制备吡非尼酮脂质体;用D-甘露糖修饰脂质体并添加适量十八胺调节脂质体表面电荷;用紫外分光光度法测定包封率;用正交实验优化处方,用透析法考察药物体外释放性质。结果：制得的脂质体平均粒径为581.1nm,表面电荷为-20.61mV,包封率为81.1%,稳定性好。药物体外释药符合Weibull方程。结论：采用薄膜分散法,用D-甘露糖修饰并添加十八胺可制得具有较高包封率及稳定性的吡非尼酮脂质体,有助于提高吡非尼酮的肺靶向性。

Study on preparation and in vitro release behavior of lung targeting perfenidone liposomes

Objective:To prepare lung targeting perfenidone liposomes and study the release of perfenidone in vitro.Method:The perfenidone liposomes were prepared by thin film method.D-mannose was used to coat the liposomes for lung targeting action and lipid membrane was modified with stearylamine.UV method was used to determine the entrapment efficiency of perfenidone liposomes.Orthogonal design was used to select the optimum formulation.Dialysis was used to study the release of perfenidone in vitro.Results:The prepared perfenidone liposomes demonstrated good stability and encapsulation efficiency was 81.1%.The average size was 581.1nm and the Zeta potential of the modified perfenidone liposomes was-20.61mV.The release in vitro was characterized by Weibull equation.Conclusion:Thin film method with freeze-thawing steps could increase the entrapment efficiency and stability of perfenidone liposomes after modification of lipid membrane with D-mannose and stearylamine.It was valuable to be further studied for lung target.