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Camptothecin(CPT) nanosuspension is prepared by anti-solvent precipitation combined with sonication with TPGS as stabilizer in our study to improve its solubility, stability and antitumor activity.Physicochemical properties of CPT nanosuspension,including particle size,polydispersity index, morphology,dissolution behavior, saturation solubility, stability and cytotoxicity assay are characterized in vitro.The pharmacokinetic evaluation is carried on the SD rats to calculate the bioavailability.And the antitumor effect of CPT nanosuspension is evaluated on MCF-7bearing mice in vivo.The particle size and polydispersity index are 204±7.6 nm and 0.235±0.081 separately.The stability and solubility of CPT nanosuspension increase significantly (P<0.01) when compared to the solution.The result of pharmacokinetic evaluation indicates CPT nanosuspension can enhance the blood concentration and relative bioavailability (146.7%).CPT nanosuspension inhibits the tumor growth significantly (P<0.01) with prolonging the survival rate compared to the solution when tested in xenografted nude mice due to increasing the accumulation of CPT in tumor issue.In summary, CPT nanosuspension will be a potentially feasible formation for tumor treatment in clinic.