Folic acid was covalently conjugated to bovine serum albumin nanoparticles (BSANP) to target the nanoparticles to SKOV3 cells expressing folate receptors. Mitoxantrone was incorporated into the folate-conjugated albumin nanoparticles, and the final nanoparticle size was 68 nm, as measured by a laser light scattering particle analyzer. The cytotoxic activity of mitoxantrone-loaded, folate-conjugated albumin nanoparticles (MTO-BSANP-folate), which was quantitated by $^3H$-thymidine incorporation, was higher than mitoxantrone-loaded BSANP(MTO-BSANP) and MTO solution, and could be inhibited by free folic acid. MTO-BSANP-folate may be endocytosed via the folate receptor on the surface of SKOV3 cells. MTO-BSANP-folate also inhibited tumor growth better than the MTO-BSANP and MTO solution in vivo. These results indicate that folate-conjugated BSANP may have therapeutic potential as a vector for anticancer drugs in cancer chemotherapy.