对氧磷酶长循环脂质体的制备及评价

Preparation and Evaluation of Long-circulating Liposomes of Paraoxonase

目的研制对氧磷酶长循环脂质体。方法采用薄膜分散法制备对氧磷酶长循环脂质体,采用凝胶柱法测定包封率,以包封率为指标,分别考察药脂比、胆固醇用量、聚乙二醇-胆固醇用量、离子强度等对脂质体的影响,在此基础上用正交设计对处方进行优化。结果经薄膜分散法制得的脂质体包封率为(87.66±3.46)%,平均粒径为126nm左右,粒度分布均匀,呈单峰分布,电镜结果显示外形圆整,分散性较好。4℃放置15d包封率无明显变化,酶活性基本稳定。结论聚乙二醇修饰的对氧磷酶长循环脂质体制备工艺简单可行,对氧磷酶长循环脂质体制剂学、酶学性质稳定。

Objective To prepare the long-circulating hposomes of paraoxonase （PON）. Methods The long-circulating liposomes of pamoxonase were prepared by film dispersion method. The encapsulation efficiency was determined by gel column. The effects of the factors on the encapsulation efficiency, such as the weight ratio of paraoxonase to phospholipid, cholesterol （Chol） to phospholipid, PEG-cholesterol （PEG-Chol） and the iron strength of water phase, were investigated respectively. Then the formulation was optimized by otthogonal design. Results The encapsulation efficiency of the paraoxonase lipesomes was 87.66_＋3.46 % ,and the average diameter of the liposomes was about 126 nm. There was no significant change on encapsulation efficiency on 15 d at 4℃ ,and the activity of paraoxonase was maintained basically stable. Conclusion The preparation of PEG-modified pamoxonase liposomes was easy and practicable, and the property investigation in vitro showed that the paraoxonase lipesomes were stable.