Objective: To study on the pharmacokinetics of chlorin e6(Ce6) phosphate-buffered saline(PBS) solution and its liposomes in tumor-bearing mice

and to verify the liver and tumor targeting of Ce6 liposomes. Method: After Ce6 solution or its liposomes were injected into tail vein of tumor-bearing mice

at different time points

the drug concentrations in serum and tissues of tumor-bearing mice were determined by HPLC

and the pharmacokinetic parameters were calculated by DAS 2.1.1 software

while the relative uptake rate(RE) within 8 h was adopted to calculate the targeting performance of Ce6 on the main organs. Result: The pharmacokinetic models of Ce6 solution and its liposomes in plasma of tumor-bearing mice were consistent with the two-compartment model

their half time of distribution phase(t1/2α) were 1.516 h and 0.507 h;their half time of elimination phase(t1/2β) were 0.457 h and 1.366 h;clearance rates(CLs) were 0.178

0.067 L·h-1·kg-1; their AUC0-∞ were 16.734

51.475 mg·h·L-1

respectively.In liver

spleen and tumor tissues

the RE values were 1.149

1.477 and 1.277

respectively.The statistical analysis showed that there was a significant difference in major pharmacokinetic parameters between Ce6 solution and Ce6 liposomes(P<0.05). Conclusion: Compared with Ce6 solution

Ce6 liposomes has a more slowly metabolic clearance in vivo

and it distributes more rapidly and widely

it also can selectively assemble in liver and tumor tissue

liposomal formulations of Ce6 may be further developed for the treatment of liver cancer.