Alzheimer's disease (AD), the most common form of dementia, is now representing one of the largest unmet medical needs. However, no effective treatment is now available to impede the progression of AD or delay its onset. There are two major challenges for the development of effective therapy for AD. First, the exact cause for AD onset is still unknown. Second, brain drug delivery is significantly hindered by the blood-brain barrier (BBB). In this review, we will summarize the pathological understanding about AD and the related treatments, compare BBB and its effect on brain drug delivery under normal and AD conditions and review the nanotherapeutic strategies that have been developed for AD therapy in recent years.