豆磷脂替代卵磷脂制备碘醚柳胺脂质体研究

The study on preparation of rafoxanide liposomes made by soybe an lecithin instead of lecithin

采用改良的冷冻溶融法 ,用豆磷脂替代卵磷脂制备了碘醚柳胺 (Rafoxanide,Raf)脂质体 ,并对其药物特性进行了测定与观察。用此法制备出的碘醚柳胺豆磷脂脂质体包封率高达 57.54 %。电镜下显示碘醚柳胺脂质体以多层脂质体为主 ,粒径大多分布在 0 .1～ 1 .0 μm之间。室温条件下贮存 75d后 ,其包封率由原来的57.54 %下降到 52 .32 % ,提示用豆磷脂脂质体具有良好的稳定性。分别按 0 .1 5mg kg ,0 .3mg kg ,0 .6mg kg体重剂量给肝片吸虫病患羊皮下注射碘醚柳胺脂质体 ,3d后剖杀 ,发现 0 .3mg

Rafoxanide (Raf) liposomes made by soybean lecit hin instead of lec ithin were prepared by modified freeze-thawing method and its characteristics and curative effects to fascioliasis had been observed. The encapsulated rate of Raf-Spc-liposomes was up to 57.54%. Observed by TEM an dmeasuredbycentrifuge,mostofves iclesweremultilamellarandthesize rangingfrom0.1to 6.0 μm h ad been found, most of which rang from 0.1～1.0 μm. The encapsulated rate dropp ed from 57.54% to 52.32% when Raf-Spc-liposomes were stored in room temperatur e for 75 days. Compared with lecithin,Raf-liposomes made by soybean lecithin had more stability. To determine the killing action of Raf liposomes to Fasciola hepatica,which made from lecithin and soybean lecithin, three sheep in each group infected naturally with Fasciola hepatica were administrated by subcutaneous injection at the same dosage of 0.15,0.3,0 .6 mg/kg body weight respectively. All sheep were dissected 3 days later. The r esults showed that all parasites had been di ed in the group of 0.3 mg/kg and 0.6 mg/kg body weight,which indicated that Rafo xanide-Spc-liposomes will be an ideal drug for fascioliasis in the future.