The vastness and multidimensional adversity of Alzheimer's disease (AD) impede the outgrowth of its therapeutic research. Needless to say, the application of nanoscience has amplified the progress of prophylaxis and therapeutics development for AD. In this Review, we will elaborate on the advancement of a nanoparticlebased alternative therapeutic targeting AD in terms of design, approach, mechanism of action, and limitations associated with their clinical availability. So far, the blood−brain barrier (BBB) is one of the major hurdles for the clinical application of drugs for any neurodegenerative disease. Here, we will focus on the current stateof-the-art of nanoparticle-based therapeutics for crossing the BBB.