Preparation and Pharmacokinetics of Vinorelbine Bitartrate Liposomes in Rats

Vinorelbine bitartrate(1) liposomes were prepared by reverse-phase evaporation combined with freeze-drying method. The properties and pharmacokinetics of the product were investigated. The results of transmission electron microscopy(TEM) showed that the product was almost spherical. The mean diameter and entrapment effi ciency of 1 liposomes were(221.5±19)nm and(86.7±1.0)%. The cumulative release at 24 h of 1 from the liposomes was about 83.4%. The pharmacokinetic behaviors of 1 solution and its liposomes in rats after intravenous administration were evaluated. The main pharmacokinetic parameters were as follows: t1/2?(0.09±0.03) and(0.32±0.10)h, t1/2?(1.45±0.21)and(4.00±0.25)h, AUC0→t(2.44±0.12) and(37.75±0.98)mg·h·L-1, AUC0→∞(2.71±0.52) and(38.16±0.98)mg·h·L-1.