The paper initially focuses on the characteristics of Polyvinyl Alcohol (PVA) hydrogel as smart delivery media, such as chemical stability, biocompatibility, and capacity for controlled release of bioactive compounds. Then, it discusses the effect of loading bioactive compounds into PVA hydrogel, considering their stability of delivery media, controlled release, and targeted delivery, enhancing therapeutic outcomes. Loading bioactive compounds such as diphlorethohydroxycarmalol (DPHC), curcumin, carotenoids, andrographolide, and flavonoids into PVA hydrogels can enhance biomedical functionalities. These functionalities include improved drug delivery, wound dressing efficacy, tissue engineering potential, and contact lens applications. Further, while previous review papers have extensively covered aspects such as the source of bioactive compounds, extraction methods, synthesis of PVA hydrogel, and various biomedical applications, there remains a gap in the literature in which no studies have systematically explored the loading of bioactive compounds into PVA hydrogel. This targeted investigation distinguishes our work from previous studies and contributes a novel perspective to the expanding hydrogel market. In light of the projected compound annual growth rate of 7.15% in the hydrogel market from 2021 to 2028, this study provides a pioneering overview of recent advancements in bioactive compound-loaded PVA hydrogels. Finally, this review outlines the challenges in optimizing bioactive compound-loaded PVA hydrogels' performance and their biomedical application. In the future direction, this review explores their potential in smart delivery media, such as optimizing the loading efficiency and releasing kinetics to specific target therapeutic, crosslinking with double or triple network hydrogels, and convergence of nanotechnology with hydrogel that become frontiers in precision medicine.