Study on pharmacokinetics of folic acid coupling nanometer paclitaxel liposome in rats

Objective To study the pharmacokinetics of folic acid coupling nanometer paclitaxel liposome in rats.Methods Rats plasma was extracted,preprocessed and then analysed after paclitaxel liposome and folic acid coupling nanometer paclitaxel liposome was injected.HPLC-UV was used to determine the plasma drug level in rats,and excel software was used in drawing the plasma concerntration-time curves,drug and statistics(DAS) software in calculation of compartment model and pharmacokinetics parameters.Results ① Linearity was confirmed over the whole calibration range from 0.07μg/ml to 30μg/ml(r=0.9998).The intra-and inter-day precisions(RSD)of analysis were lower than 6%.The extraction recovery at three different concentration(10.0、2.0、 0.2μg/ml)was better than 90%.② The concentration-time profile for folic acid coupling nanometer paclitaxel liposome injection could be best described by three-compartment model fitted by 1/C2 weight and paclitaxel liposome injection was described by two-compartment model fitted by 1/C2 weight.③ T1/2α,T1/2βof folic acid coupling nanometer paclitaxel liposome were(0.12±0.10)h and(0.40±0.08)h,t1/2γwas(3.29±1.02)h,CL was(1.37±0.04)L/(kg·h),AUC(0~t),AUC(0~∞)were(12.19±0.40)mg/(L·h)and(14.61±0.40) mg/(L·h),while T1/2αof paclitaxel liposome was(0.09±0.08)h,T1/2βwas(2.57±0.51)h,CL was(1.50±0.10)L/(kg·h),AUC(0~t)and AUC(0~∞)were(9.30±0.48)mg/(L·h),(13.39±0.92) mg/(L·h).④ The t-test results show that the elimination half-life time,CL,AUC(0~t),AUC(0~∞)were all statistically significant.Conclusion Folic acid coupling nanometer paclitaxel liposome can be distributed in the whole body and achieve balance fast,last for a longer time,and have higher bioavailability.