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目的采用甲氧基聚乙二醇磷脂酰乙醇胺(mPEG-DSPE)修饰紫杉醇脂质体,并考察其在大鼠体内的药动学行为。方法合成两亲线型聚合物mPEG-DSPE;采用薄膜分散法制备mPEG-DSPE修饰的紫杉醇脂质体;并用HPLC测定紫杉醇在大鼠体内的血药浓度。结果得到的紫杉醇脂质体粒径为(411.8±31.9)nm,包封率为(82.47±2.15)%。紫杉醇注射液和修饰后脂质体的t1/2β分别为1.48和10.48h,后者AUC约为前者的3.13倍。结论mPEG-DSPE修饰的紫杉醇脂质体具有显著的长循环特性,并可提高其体内的利用度。
OBJECTIVE To prepare the paclitaxel liposomes modified with mPEG-DSPE and study its pharmacokinetics in rats.METHODS The mPEG2000-DSPE was synthesized and used to modify the lipid membrane.The paclitaxel liposomes were prepared by a thin-film dispersion method.The concentration of the paclitaxel in rat plasma was determined by HPLC method.RESULTS The particle size of the resulting paclitaxel liposomes was(411.8±31.9)nm,and its encapsulation was(82.47±2.15)%.Pharmacokinetic study showed that t1/2β of paclitaxel injection and paclitaxel liposomes were 1.48 and 10.48 h,respectively.The AUC value of the liposomes was increased.The AUC of liposomes was 3.13 times as that obtained after i.v.administration of the paclitaxel injection.CONCLUSION The in vivo circulating time of the paclitaxel liposomes modified with the mPEG-DSPE could be lengthened,and the AUC has been improved in some extent.
