Abstract Microspheres formulated from poly (D, L-lactic-co-glycolide) (PLGA), a biodegradable polymer, have been extensively evaluated as a drug delivery system. In this study, the preparation, characterization and drug release properties of the PLGA microspheres were evaluated. Simvastatin (SIM)-loaded PLGA microspheres were prepared by oil-in-water emulsion/solvent evaporation method. The microspheres were then frozen to −80 °C, they were freeze dried for 24 h. Characterization of SIM-loaded PLGA microspheres was evaluated by X-ray diffraction analysis, Fourier transform infrared spectroscopy analysis, and scanning electron microscopy (SEM). Drug release potential was evaluated by UV-spectrophotometry. The experimental results revealed that SIM-loaded PLGA microspheres can be successfully obtained through solvent evaporation method with appropriate morphologic characteristics and high encapsulation efficiency. The drug release pattern from polymeric microspheres in the phosphate buffered saline medium was measured during a 21-day period using UV-spectrophotometry. The correlation coefficient value (r 2 = 0.9878) of the trend lines of the graph showed that the SIM-loaded PLGA microspheres best fit with zero order release pattern. No burst release was observed with polymeric matrix. The drug release characteristic of the microspheres ascertained that the release was about 27% for SIM-loaded microspheres, which occurred within the first 6 days after maintaining the microspheres in phosphate buffer saline. Also, the microspheres successfully presented a slow release and the duration of the release lasted for more than 21 days. It can be concluded that SIM-loaded PLGA microspheres hold great promise for using as a drug-delivery system in biomedical applications, especially in drug delivery systems and tissue engineering