Anticancer drug release from polylactic acid microspheres prepared by the spray-drying process was studied. Several process parameters and properties of the polymer solution have been investigated. Normal size distributions with diameters ranging from 5-10 mum were obtained by the spray drying technique. The yield of microspheres recovered depended on polymer solution and process conditions employed. Results show that the yield of microspheres could reach 50%, and the experimental drug loading approached the theoretical drug loading. Scanning electron microscopy indicated that microspheres were composed of a dense thin skin layer and porous core. The magnitude of this effect depended on the inlet temperature, feed polymer concentration and airflow rate. Increasing inlet temperature and polymer concentration resulted in an intact particle shape and a slower drug dissolution rate. The in-vitro release of anticancer drug from microspheres was sustained over 7 days. The drug release behaviour depended on inlet temperature, air flow rate, PLA concentration and drug loading. The anticancer drug release rate from polylactic acid microspheres prepared by the spray-drying method was depressed, and the long-acting release could be achieved by appropriate operating parameters.