【摘要】 目的制备长效利拉鲁肽多囊脂质体(liraglutide-load multivesicular liposomes,Lrg-MVLs),并对其理化性质和体外释放进行了考察。方法采用复乳法制备Lrg-MVLs,以成形性、粒径为评价指标,采用单因素试验优化Lrg-MVLs制备条件。测定了优化处方制备的Lrg-MVLs包封率和粒径,并考察了其体外释放度。结果优化处方制备的Lrg-MVLs平均粒径为8.23μm,包封率为(88.69±0.65)%。体外释放结果显示,Lrg-MVLs体外持续释放达168 h,2 h释放(1.18±0.77)%,无突释现象,体外释放符合Ritger-Peppas模型。结论 Lrg-MVLs呈典型的非同心圆结构,粒径均匀、包封率高,可用于包载Lrg(liraglutide)达到缓慢释放的目的。更多还原

【Abstract】 Objective To prepare a long-acting liraglutide-loaded multivesicular liposomes(Lrg-MVLs),and to evaluate the physicochemical properties and in vitro release of Lrg-MVLs.Methods Lrg-MVLs were prepared by the double-emulsion method.The formulation and preparation process were screened and optimized after single factor experiment with the index of formability and particle size.Then the particle size and encapsulation efficiency of Lrg-MVLs were measured.Meanwhile,in vitro release of Lrg-MVLs was evaluated.Results The mean particle size of Lrg-MVLs was 8.23 μm with a high encapsulation efficiency of(88.69±0.65)%.The Lrg loaded Lrg-MVLs exhibited a sustained release over a period of 168 h,and the cumulative release amount of 2 h was(1.18±0.77)%,which indicated that Lrg-MVLs had no initial burst.The results of fitting equations and coefficients were fitted to the model of Ritger-Peppas.Conclusion Lrg-MVLs have a typical structure of non-concentric multiple lipid layers with a high encapsulation efficiency,which can be suitable for the sustained release of Lrg.更多还原