超氧化物歧化酶脂质体在大鼠体内的药代动力学和组织分布

目的考察3种超氧化物歧化酶(SOD)脂质体静脉给药后在大鼠体内的药代动力学和组织分布。方法 用反相蒸发法制备SOD脂质体，采用黄嘌呤氧化酶法检测SOD活力，静脉注射给药后，测定大鼠血中SOD含量变化和不同组织中SOD含量变化。结果在血浆中，SOD水溶液、SOD普通脂质体、用DSPE-PEG2000修饰的SOD脂质体、用Tween 80修饰的SOD脂质体的半衰期分别为0.25，0.34，0.66和0.41 h；AUC分别为12.48，24.66，41.16和33.02 μg·h·mL^-1。与普通脂质体比较，经过DSPE-PEG和Tween 80修饰后的脂质体，使肝、脾中SOD的含量有不同程度的降低，脑中含量有所提高。结论3种SOD脂质体均可不同程度地延长SOD的血浆半衰期，并以用DSPE-PEG2000修饰的SOD脂质体效果最好。与普通脂质体相比，用Tween 80修饰的SOD脂质体可以提高进入脑中的SOD量，用DSPE-PEG2000修饰的SOD脂质体可以减少肝脾对SOD的摄取。

Pharmacokinetics and distribution of superoxide dismutase liposomes in rats

AIM: To evaluate the effects of surfactants on the pharmacokinetics and distribution in rats after intravenous administration of SOD liposomes. METHODS: The liposomes were prepared by reverse phase evaporation method. The activity of SOD was assayed by method of xanthine oxidase. RESULTS: The T1/2 of SOD solution, common SOD liposome, SOD liposomes modified by DSPE-PEG2000 and Tween 80 were 0.25, 0.34, 0.66 and 0.41 h, respectively; AUC were 12.48, 24.66, 41.16 and 33.02 microg x h x mL(-1), respectively. Compared with the common liposome, the liposomes modified by DSPE-PEG and Tween 80 decreased the content of SOD in liver and spleen, but increased in brain. CONCLUSION: The three kinds of liposomes could increase T1/2 and AUC in some extent, especially in PEG-L group. Tween-L could increase the SOD content in brain, and PEG-L could decrease the SOD content in the liver and spleen compared with the common liposome.