Aim The present work aimed at the DIM-loaded microparticles development and anti-hypernociceptive action evaluation. Method The formulations were prepared by O/W solvent emulsion-evaporation method and characterised by particle diameter, content and DIM encapsulation efficiency, drug release profile, thermal behaviour and physicochemical state. The anti-hypernociceptive action was evaluated in the animal model of acute inflammatory pain. Result The MPs had a mean diameter in the micrometric range (368 +/- 31 mu m), narrow size distribution, DIM content of 150 mg/g, encapsulation efficiency around 84% and prolonged compound release. Evaluations of the association form of DIM to MPs demonstrated the feasibility of the systems to incorporate DIM and increases its thermal stability. An improvement in the anti-hypernociceptive action of DIM was observed by its microencapsuation, because it was increased and prolonged. Conclusion Therefore, the MPs developed represent a promising formulation for oral administration of the DIM in the treatment of inflammatory pain.