title: Pharmacokinetics and tissue distribution of iv injection of polyphase liposome-encapsulated cisplatin (KM-1) in rats.
abstract: OBJECTIVE
  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-1 4.5 mg/kg in rats was fitted with an open three-compartment model. The pharmacokinetic parameters were as follows: Vc=0.10 L/kg, T1/2pai=0.3 h, T1/2alpha=3.5 h, T1/2beta=2.7 h, AUC=265 mg.h.L(-1), and CL(s) =0.02 g.L.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.
  
  
  CONCLUSIONS
  KM-1 remained in the bloodstream longer than its free drug, and was taken mainly by the reticuloendothelial system.
authors.affiliation: College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China. wangshan420@163.net
authors.forename: Shan
authors.initials: S
authors.lastname: Wang
authors.forename: Jie-Bo
authors.initials: JB
authors.lastname: Mi
authors.forename: Yuan-Zong
authors.initials: YZ
authors.lastname: Li
authors.forename: Wen-Bao
authors.initials: WB
authors.lastname: Chang
authors.forename: Yun-Xiang
authors.initials: YX
authors.lastname: Ci
authors.forename: Min-Zheng
authors.initials: MZ
authors.lastname: Zhao
authors.forename: Yun-Kun
authors.initials: YK
authors.lastname: Zhao
authors.forename: Li-Ya
authors.initials: LY
authors.lastname: Zhu
authors.forename: Guang
authors.initials: G
authors.lastname: Xu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002945:Cisplatin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004337:Drug Carriers; D007275:Injections, Intravenous; D008081:Liposomes; D008099:Liver / Q000378:metabolism; D008297:Male; D010984:Platinum / Q000032:analysis / Q000097:blood; D051381:Rats; D017208:Rats, Wistar; D013154:Spleen / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008081:Liposomes; D010984:Platinum; D002945:Cisplatin