Citrus fruits are celebrated for their rich composition of bioactive compounds, including flavonoids, phenolic acids, carotenoids, ascorbic acid, and essential oils, which are associated with numerous health benefits such as antioxidant, anti-inflammatory, anticancer, and neuroprotective effects. However, the bioavailability and stability of these phytochemicals are compromised due to degradation during processing and digestion. This comprehensive review systematically examines innovative delivery methods, particularly nanotechnology-based carriers like nanoparticles, nanoemulsions, and encapsulation techniques, designed to enhance citrus bioactive absorption and therapeutic potential. We explore cutting-edge technologies that improve these compounds’ nutritional integrity and functional properties while addressing the challenges related to their bioavailability. In vivo studies indicate that nanoparticle-based formulations markedly enhance the bioavailability of citrus bioactives. Specifically, phytosomal formulations of hesperidin and hesperetin have been shown to increase peak serum concentrations (Cmax) following oral administration, whereas nanoemulsion systems facilitate improved solubilization and intestinal transport of lipophilic compounds via micelle formation. By synthesizing recent findings from pharmacological, nutritional, and food science research, this review illuminates pathways for optimizing the health benefits of citrus-derived chemicals. We also discuss the implications for future research and the potential applications of these delivery systems in personalized medicine and nutraceuticals, advocating for a paradigm shift in the development and consumption of citrus products to maximize their health benefits.