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Ischemic cerebral stroke is a leading cause of death and disability globally. At present, thrombolytics, such as recombinant tissue-type plasminogen activator, are the only effective treatment for acute stroke. Howev-er, usage of thrombolytics has a strict therapeutic window and cannot be applied to a number of patients. Despite the promising effects of some neuroprotectants in preclinical studies, they failed in clinical trials as a result of poor phar-macokinetic properties, particularly with regard to solubil-ity and permeability across the blood-brain barrier (BBB). Approaches for delivering these drugs by nanotechnologies may overcome these pharmacokinetic deficits and enhance their neuroprotective effects. However, issues such as po-tential side effects and biosafety properties currently limit clinical application of these approaches. In this article, we reviewed recent progress of nanotechnology-based inter-ventions for stroke treatment, and in particular, summa-rized novel materials applied to synthesize nanocarriers, encapsulation with neuroprotectants, and factors impacting nanodrug bioactivities to provide a theoretical basis for the development of anti-stroke drugs.