Distribution of Fluorouracil Liposomes in Mice in Vivo and Evaluation of Its Targeting Performance

OBJECTIVE: To study the distribution of fluorouracil liposomes (FU-Lip) in mice in vivo and to evaluate its targeting performance.METHODS: 90 mice were randomly divided into 10 groups.The former 5 groups were treated with intravenous injection of FU-Lip,the latter 5 groups were treated with FU injection (25 mg·kg-1 of FU).The concentrations of FU in mice plasma,heart,liver,spleen,lung and kidney were determined by HPLC respectively.The distribution of fluorouracil in tissue was analyzed.The target ability of fluorouracil to main organs was evaluated by the relative tissue exposure (re=AUCliposome/AUCinjection)and targeting efficiency(te=AUCtissue/AUCplasma).RESULTS: The concentrations of FU in tissues increased firstly then decreased.Compared with FU injection,the average concentration of FU in liver and spleen increased 24 h after intravenous injection of FU-Lip,while that of other tissues decreased.The re of FU-Lip in liver reached 17.13 while that of other tissues was lower than 7.017.The value of te1/te2 in liver and spleen were 5.616 and 2.301.That of other tissues was lower than 1.CONCLUSION: FU-Lip can increase the distribution of FU in liver and spleen with liver and spleen targeting property,especially liver targeting property.