Parkinson's disease is a neurodegenerative disorder characterized by progressive loss of dopaminergic neurons in the substantia niara. Levodopa remains the most effective drug in the treatment of Parkinson's disease. Unfortunately, with disease progression, levodopa reduces Parkinsonism at the cost of evoking abnormal involuntary movements known as levodopa-induced dyskinesia (LID). In this study, we found that levodopa/benserazide-loaded biodegradable microspheres reduce the expression of LID, which was easily evoked by administrating of the same dose of levodapa and benserazide in rats with Parkinson's disease. Moreover, levodopa/benserazide-loaded biodegradable microspheres can improve the stepping of the lesioned forepaw in rats with Parkinson's disease. These data showed that levodopa/benserazide-loaded biodegradable microspheres might be useful in the treatment of Parkinson's disease and reducing the expression of LID in rats.