The goal of the present investigation was to formulate and evaluate chitosan nanoparticles of temoxifen citrate for cancer therapy. Nanoparticles of TMX were prepared using chitosan using ionic gelation method. The concentration of the polymers Chitosan were selected based on the results on preliminary screening. The nanoparticles prepared were evaluated for morphology, loading efficiency, invitro release and invitro anticancer activities. The particle shape and morphology of the prepared TMX nanoparticles was determined by SEM analysis. The amount of TMX entrapment in the nanoparticles was calculated by the difference between the total amount of drug added to the nanoparticle and the amount of non entrapped drug remaining in the aqueous supernatant. A diffusion cell was used to monitor TMX release from the nanoparticles. The formulations FM-1 showed good drug release from the polymer. The percentage cumulative drug release after 3,4,5,6,7 and 8 hours was 40.54, 48.68, 56.26, 65.84, 71.42 and 78.03% respectively. Among the all formulations FM 1 showed maximum drug release in 8 hours diffusion study and good entrapment efficiency.