Alzheimer’s disease (AD) is the ultimate cause of cognitive decline in older adults, involving a steady deterioration of mental function. The main pathological hallmarks of AD include Aβ plaques (extracellular) and hyperphosphorylated tau protein (Intracellular). Several risk factors, such as genetics, aging, diet, cerebrovascular diseases, obesity, and inflammation, strongly show their impact on AD progression. On the other hand, inflammation and immune disorder also significantly impact BBB integrity, further exacerbating the disease progression. However, no specific treatment that can reverse the disease has been reported, and the current treatment strategies target only symptoms. This underscores the urgent need for an ideal drug treatment that can completely reverse the disease. Resveratrol, a bioactive polyphenol extracted from grapes and wine, has shown neuroprotective effects by enhancing the antiaging and antioxidant potentials and inhibiting inflammation in multiple models of AD. In addition, this compound also showed an impact on Aβ aggregation and clearance. However, resveratrol’s poor bioavailability remains challenging, necessitating novel strategies to improve its pharmacokinetic properties. This chapter highlights the multiple mechanisms of resveratrol in modulating AD pathobiology, its role in preserving BBB integrity, and its potential role in therapy.