Distribution in the body of targeted ursolic acid liposomes and their inhibitory effect on mice transplanted tumor / 中国药学杂志

ABSTRACT

OBJECTIVE: To study the distribution of folate receptor targeted ursolic acid liposomes and evaluate its antitumor effects on human epidermoid carcinoma xenografts in nude mice. METHODS: Folate derivative was used as targeting molecule and conjugated with mPEG-DSPE for obtaining liposome with long circulation features. This novel targeted agent was prepared by a thin-film dispersion method and ursolic acid was loaded into the liposomes as the anticancer drugs. Tissue distribution of liposomes in heart, liver, spleen, stomach, kidney and tumor were investigated. The antitumor effect of the targeted ursolic acid liposomes (F-PEG-L-UA) on human epidermoid carcinoma xenografts in nude mice was also studied. RESULTS: Compared with free ursolic acid liposome, UA liposome was slowly removed from blood circulation and the concentration of F-PEG-L-UA in liver, kidney and tumor tissue is significantly higher than other groups. The growth speed of tumor in the group of F-PEG-L-UA was significantly slowed down compared with other groups. The tumor volume in F-PEG-L-UA group was about 50% reduction compared with PBS-treated mice (P<0.05). CONCLUSION: A novel targeted ursolic acid compound is synthesized as the folate receptor targeting functional material. It has obvious inhibitory effect on human epidermoid carcinoma xenografts and it might be an effective antitumor drug delivery system.