Alzheimer's disease (AD) is a very common progressive and destructive degenerative disease of the central nervous system that affects the quality of life of the elderly and poses a serious risk to their lives, placing a huge economic burden on families, society and the state. There are not many breakthroughs as well as innovations in current medications for the treatment of AD, and there is also the challenge of breaking through the blood-brain barrier, and improper treatment may lead to adverse reactions in patients. Targeted drug delivery system, as an effective therapeutic modality, can significantly reduce the concentration of drugs in the blood, the frequency of drug delivery and the drug toxicity, while increasing the concentration and efficacy of drugs at the target site and drug bioavailability, as well as providing a slow-release effect for drugs. In addition, the targeted drug delivery system is also expected to penetrate the blood-brain barrier, improve blood-brain penetration, realize brain targeting, and deliver drugs precisely, thus providing an efficient and safe way to treat AD. This work reviews the pathogenesis of AD, the non-pharmacological methods of adjuvant drug therapy for the treatment of AD as well as the mechanism of action and side effects of the main drugs targeting amyloid β protein (Aβ) aggregation, acetylcholinesterase inhibition, and receptor antagonism, etc. It also briefly introduces and combs through as well as summarizes the targeting drug delivery systems for the treatment of AD such as magnetic nanoparticles, liposomes, and so forth, points out the problems that exist at the moment, puts forward the possible solutions, and indicates the direction of possible development in the future.