Resveratrol (RES) is a stilbene group of natural polyphenolic compounds in trees, peanuts, and grapes. RES is revealed with anticancer, antioxidant, anti-inflammatory, and cardioprotective effects. Though it is proven with prominent therapeutic activity, low aqueous solubility, poor bioavailability, and short half-life had hindered its use to exploit the potential. Also, the first-pass metabolism and undergoing enterohepatic recirculation are obscure in the minds of researchers for their in vitro studies. Many approaches have been investigated and shown promising results in manipulating their physicochemical properties to break this barrier. Nanocarriers are one of them to reduce the first-pass metabolism and to overcome other hurdles. This article reviews and highlights such encapsulation technologies. Nanoencapsulated RES improves in vitro antioxidant effect, and this review also highlights the new strategies and the concept behind how resveratrol can be handled and implemented with better therapeutic efficacy.