配体介导多烯紫杉醇脂质体大鼠体内药动学和小鼠组织分布研究

Objective: Compare the pharmacokinetics parameters of rats and tissue distribution in mice injected with docetaxel liposomes modified with cholesterol-galactose, conventional liposomes and docetaxel injection to study the pharmacokinetics of docetaxel liposomes modified with cholesterol-galactose ligand injection in rats. Methods: Compare the pharmacokinetics parameters of G-DOC-L with DOC-L and DOC-i by injected intravenously with single dose of 5.0 mgokg-1 in rats. The blood samples and tissue samples were collected at the designed time points, and DOC concentrations were measured by LC-MS/MS. DAS2.0 was used to calculate the pharmacokinetics parameters. Results: The results indicated that the t1/2z of DOC-i group, DOC-L group and G-DOC-L group was 4.35、2.97 and 3.39h, respectively, with CL was 1.52, 1.09 and 4.19 Loh-1okg-1, respectively. The hepatic uptake rate was 21.64%, 10.740% and 7.660%. The renal uptake rate was 21.64%, 10.740%, 7.660%. Conclusion: These results indicated that G-DOC-L can remarkably reduced the blood exposure and have high hepatic uptake rate and low renal uptake rate. G-DOC-L has a specific target to liver.