Abstract��
OBJECTIVE To prepare lomustine(CCNU) liposomes and study their pharmacokinetics in rats after intravenous administration.METHODS To prepare CCNU liposomes by improved reverse-phase evaparation method.The entrapment efficiency and mean diameter were studied.After intravenous administration,the CCNU in plasma was detected by HPLC and the pharmacokinetic parameters were calculated by 3P87 pharmacokinetic program.RESULTS The entrapment efficiency of CCNU liposomes was above 80% and the mean diameter was about 50 nm.The t1/2�� of CCNU solution,common CCNU liposomes,CCNU liposomes modified by PEGCHS were 0.061 8,0.093 1 and 0.153 1 h,respectively;t1/2�� were 0.087 9,0.416 2 ��1.002 1 h,respectively;AUC were 13.520 7,86.911 3 and 166.640 6 mg��h��L-1,respectively.CONCLUSION The CCNU liposomes have high entrapment efficiency and small particle size.The two kinds of liposomes raise the AUC and prolonge the resident time of the drug in the blood circulating system,especially in PEG-L group.
2007, Vol. 42 