Introduction: The aim of this study was to develop an optimized formulation for labeling a third-generation bisphosphonate, zoledronic acid with [99m(TC)] (TC) to achieve the best formulation in preparing an ideal skeletal radiotracer. Radiocomplex yield and purity, stability, biodistribution and imaging in normal rat were investigated. Methods: The samples containing different amounts of zoledronic acid, ascorbic acid and stannous chloride were prepared and labeled with [ 99m (TC)]technetium pertechnetate. TLC methods were used to determine the radiochemical purity. The stability was determined in saline and human serum solutions. Lipophilicity was calculated by measuring radio-complex that was divided between organic and aqueous phases. In vitro bone affinity was studied through hydroxyapatite binding assays. Considering the decomposition of radioactivity, biodistribution of radio-complex was assessed based on the percentage of injected activity per gram of organ (% IA/g). Results: [99m(TC)](TC)-zoledronic acid was prepared easily with high yield while 100 µ, g, 0. 34 µ, mol of zoledronic acid as a ligand and 100 µ, g, 0. 44 µ, mol SnCl2 as a reducing agent were used. Radiochemical purity of radio-complex was more than 99% with specific activity of 8050 MBq/µ, mol. The radio-complex showed rapid blood washout along with high bone uptake value (4. 53 ±,0. 14 % IA/g at 2 h post injection). Conclusion: Under optimized condition, [99m(TC)](TC)-zoledronic acid was prepared with high purity and stability together with high bone affinity and rapid blood clearance, make this radio-complex an ideal agent with great potential for skeletal imaging.