Plant polyphenols and polyphenol-rich extracts are known to exhibit a wide range of anti-cancer, anti-inflammatory, anti-oxidative and pro-apoptotic properties, and may also suppress the development of many ophthalmological diseases. Dry eye disease is associated with disturbances of the tear film. Although synthetic drugs and artificial tears can be used to treat the disorder, their long-term use may cause many side effects. The etiology of dry eye syndrome is complex, but the disease is now recognized as being mainly associated with ocular surface inflammation and oxidative stress. This review highlights the impact of polyphenols (alone or mixed) on the inflammatory process contributed to the pathophysiology of dry eye syndrome and summarizes the scientific basis for this action. It also describes the preclinical development, pharmacological properties, clinical efficacy and safety of polyphenols.