PEG修饰鳖甲肽HGRFG脂质体的药动学研究

Study on Pharmacokinetics of PEG-modified Trionycis Carapax Peptide HGRFG Liposome

目的制备鳖甲肽HGRFG脂质体以及聚乙二醇(polyethylene glycol,PEG)修饰后的长循环脂质体,考察经修饰的脂质体较未修饰脂质体在动物体内分布及滞留情况。方法采用BLB/c裸鼠荧光活体成像实验,进行脂质体体内分布及代谢研究;采用药动学实验,初步探究2种载药脂质体在血浆内的滞留时间。结果 2种载药脂质体均能广泛分布于实验动物体内。与未经修饰的脂质体载药组相比,经PEG修饰的长循环脂质体载药组中裸鼠荧光全部消失的时间明显延长,药物在血浆滞留时间也明显延长。结论经PEG修饰后的长循环脂质体可以延长药物在实验动物体内的滞留时间,延长药物半衰期。

OBJECTIVE Trionycis Carapax Peptide HGRFG liposome and its long-circulating liposome modified by polyethylene glycol(PEG) were prepared to study the distribution of modified liposomes and unmodified liposomes in animals. METHODS The BLB/c nude mouse fluorescence in vivo imaging experiment was used to study the distribution and metabolism of liposomes in vivo. The pharmacokinetic experiments were used to investigate the retention time of two different drug-coated liposomes in plasma. RESULTS Two different drug-coated liposomes were widely distributed in experimental animals. The retention time of fluorescence disappearance in nude mice of PEG-modified long-circulating liposome-packaging group was significantly higher than that in unmodified liposome-containing drug group. The retention time of the drug in the unmodified liposome group was significantly lower than that in the PEG-modified group. CONCLUSION It has been experimentally confirmed that long-circulating liposomes modified by PEG can prolong the storage time of the drug in experimental animals and prolong the half-life of the drug.