Pharmacokinetics and tissue distribution of iv injection of polyphase liposome—encapsulated cisplatin（KM—1） in rats

• Published in: Acta pharmacologica Sinica Vol. 24; no. 6; pp. 589 - 592
• Main Author: WANGShan MIJie-Bo LIYuan-Zong CHANGWen-Bao CIYun-Xiang ZHAOMin-Zheng ZHAOYun-Kun ZHULi-Ya XUGuang
• Format: Journal Article
• Language: English
• Published: 2003
• Subjects: 多相脂质体胶囊; 抗肿瘤药; 药物代谢动力学
• ISSN: 1671-4083; 1745-7254

AIM:The pharmacokinetics and biodistribution of cisplatin encapsulated in polyphase liposome (KM-1) were compared with those of free drug in rats. METHODS: The platinum levels in serum and normal organs, after a single dose of iv injection of free or encapsulated cisplatin to rats, were determined by induced coupled plasma atomic emission spectrometry. RESULTS: Serum platinum concentration-time curve after a single iv dose of KM-14.5mg/kg in rats was fitted with an open three-compartment model. The pharmacokinetic parameters were as follows: Vc=0.10L/kg, T1/2π=0.3h, T1/2α=3.5h, T1/2β=2.7h, AUC=265mg·h·L^-1, and CL(s)=0.02g·L^-1·h^-1. KM-1 was cleared from the circulation much more slowly than free cisplatin. Liver and spleen had the highest concentration of platinum after KM-1 treatment. CONCLUSION:KM-1 remained in the bloodstream longer than its free drug, and was taken mainly by the reticuloendothelial system.