碘海醇脂质体的制备及其质量评价

采用逆相蒸发法制备碘海醇脂质体。对脂质体的形态、包封率、粒径分布、体外释放及体内造影情况等性质进行研究。透射电镜下观察脂质体为粒径均匀的球状或近球状小囊泡。HPLC法测定碘海醇脂质体包封率为82.35%±1.82%。碘海醇脂质体平均粒径207.7nm,分散指数0.355,Zeta电位-1.83mV。体外释放度试验表明碘海醇脂质体中药物的释放明显比碘海醇单纯药物缓慢,24h才达到98.57%。体内试验结果表明脂质体包裹的造影剂比普通造影剂CT峰值推后,信号增强,作用时间延长。碘海醇脂质体包封率较高、重现性良好。将碘海醇包裹于脂质体后减少给药剂量、延长作用时间,并可能减小对血管和中枢神经的毒性。

Preparation and Quality Evaluation of Iohexol Liposomes

The liposomes were prepared by reverse-phase evaporation technique. The morphology of the liposomes, the entrapment efficiency and the particle size distribution were evaluated. The CT signals of Iohexol liposomes in rabbits were compared with those of Iohexol injection in rabbits. The entrapment efficiency of Iohexol liposomes was 82.35% +/- 1.82%. The liposmes were spherical or ellipsoidal shape in shape. The mean diameter of the Iohexol liposomes was 207 7 nm. The polydispersity index was 0.355. The Zeta potential was--1.83 mV. The drug was highly entrapped into the liposomes with good reproduction and stability. The in vitro release of Iohexol liposomes was significantly slower than that of Iohexol,and was 98.57% at 24 h. Iohexol liposomes may reduce the dosage, prolong the effective time of the developing agent, and could reduce the side effects of Iohexol on the blood vessels and cerebral nerves.