Ischemic stroke is the second leading cause of death and long-term disability worldwide, for which no effective therapies are available. The increasing prevalence of ischemic stroke and related health risks, combined with the lack of effective therapies, highlight the desperate need for continued research for exploring the safe and effective drugs, which favourably influence multiple pathways leading to neuroprotection and extend the benefit to a larger number of patients diagnosed with stroke. Numerous preclinical studies have reported very promising results using “neuroprotectants”, all of which have failed at clinical trials because of either safety issues or lack of efficacy. The delivery of many potentially therapeutic neuroprotectants and diagnostic compounds to specific areas of the brain is restricted by the blood-brain barrier (BBB). Nanoparticles (NPs) have colossal applications that could revolutionize the treatment of ischemic stroke. NPs can readily transmigrate across the BBB without compromising its integrity. Recent striking developments in nanotechnology have produced a great deal of nano-devices, which could be used for the treatment and neuronal regeneration following ischemic stroke. This article attempts to convey the untapped potentials of nanopharmaceuticals for the treatment of ischemic stroke. Looking towards the future, this review focuses on the potential applications of nanoparticulate systems for the delivery of therapeutic cargo into the brain for imparting neuroprotection against ischemic stroke. This review also provides an overview of targeted NPs, which are being used for imaging, neuroprotection and regeneration of ischemic brain.