Grapefruit (Citrus paradisi) is a well-known tropical hybrid citrus fruit overpowered withoverabundant in vitamin C. ItsIt's healthy, refreshing versatility is commanding of the overall wellbeing of the human body. The whole fruit, including, skin, pulp, and seeds are all utilized as a functional food and for pharmaceutical applications. It is packed with impressive nutrients including minerals and flavonoids like hesperetin, narringin, and naringenin. Although nanotechnology has reduced the adverse effects of conventional drug therapy in cancer treatment, tissue specificity is still a challenging issue. Recent trends of developing promising nanoparticles from grapefruits are in the limelight for various layers of experimentation. This is having exposure as promising anticancer agents, and its application is gaining importance over conventional carcinoma treatment. Thereby in this review, our focus is mainly on the improvement of the nutritional profile, and the conventional and modern extraction techniques of grapefruit various extracts. With thefrom grapefruit. With respect to this context, this fruit has enormous health beneficial activities like antimicrobial, antioxidant, anti-proliferative, anticancerand anticancer to treat several medical conditions. Different findings of the past decade on the metal nanoparticles process using this magical fruit’s flavones are also focused on the role of Grapefruitgrapefruit nanovectors in the internalization of anticancer drugs through various routes, including intranasal delivery to the brain. Reports on clinical and preclinical studies targeting various tumors are also highlighted. We alsoIn addition, we highlighted certain important and similar reports of the progenitors Citrus maxima, Citrus sinensis, Citrus reticulata, and Citrus grandis. Later on, our researchers suggested some very important aspects of future research of interest to enhance the therapeutic efficacy of Citrus Paradisiparadisi.