[Antitumor activity of mitoxantrone-nanosphere against murine liver tumor H22].

Objective: [corrected] To make a comparison between mitoxantrone (DHAQ) and liver targeting drug delivery system mitoxantrone-polybutylcyanoacrylate-nanosphere (DHAQ-PBCA-NS) in respect to their antitumor activity against experimental liver tumor H22 in mice.

Methods: Drugs were given intravenously on the 1st, 5th, 9th day after planting tumor respectively. Weight of tumor in mouse was determined and the results were compared with those of mitoxantrone (DHAQ).

Results: There was relationship of dose-effect for both DHAQ and DHAQ-PBCA-NS, and the median effective dose (ED50) of DHAQ and DHAQ-PBCA-NS was 1.04 mg/kg and 0.34 mg/kg respectively. The lethal dose to 50% of the population (LD50) of DHAQ and DHAQ-PBCA-NS i.v. in mice with the same administration schedule was 3.670 mg/kg and 4.225 mg/kg respectively. Therefore, the calculated value of therapeutic index was 3.53 for DHAQ and 12.43 for DHAQ-PBCA-NS. In addition, the antitumor activity of both drugs with different treatment schedules was reported. The results showed: the earlier the mice were treated, the higher the antitumor activity of the two drugs were seen. However, DHAQ-PBCA-NS presented higher activity than DHAQ did, when the same treatment schedule was followed.

Conclusion: The results demonstrated that the antitumor activity of DHAQ-PBCA-NS is much higher than that of DHAQ, and DHAQ-PBCA-NS is possessed of liver targeting property.