Citrus fruits are renowned for their rich content of bioactive compounds, including flavonoids, vitamin C, and carotenoids, which have been linked to numerous health benefits such as antioxidant, anti-inflammatory, and anti-carcinogenic properties. Traditional methods for extracting these compounds, such as solvent extraction, steam distillation, and maceration, often fall short in terms of efficiency, sustainability, and the preservation of compound integrity due to the use of high temperatures or harsh chemicals. This review paper explores the emergence of novel innovative techniques that promise to overcome these limitations, including Ultrasonic-Assisted Extraction (UAE), Supercritical Fluid Extraction (SFE), Microwave-Assisted Extraction (MAE), Pulsed Electric Fields (PEF), and Enzyme-Assisted Extraction (EAE). Each method is evaluated for its principle of operation, advantages, comparative effectiveness, and the quality of bioactive compounds extracted. The review highlights significant findings from recent studies, showcasing the superior efficiency of these novel techniques in extracting higher yields of bioactive compounds while maintaining their functional integrity and reducing environmental impact. Comparative analyses reveal the conditions under which each technique offers the greatest advantages, including considerations of cost, scalability, and applicability to different citrus types. The paper concludes with a discussion of the challenges facing the wider adoption of these techniques in the industry, such as technical limitations, cost implications, and the need for further research to optimize extraction conditions for industrial-scale operations. Future research directions are suggested, emphasizing the potential of integrating these novel techniques into existing processing lines to enhance the sustainability and efficacy of citrus bioactive compound extraction. This chapter provides a comprehensive overview for researchers, technologists, and industry professionals seeking to harness the nutritional and medicinal potential of citrus fruits through more efficient, sustainable, and effective extraction methods.