Acoustic cavitation-based drug delivery systems were gaining more interest by the researchers in recent years and emerged as a transformative approach in modern medicine, offering noninvasive, precise and targeted delivery of drug. By utilising ultrasound waves, these systems enable the efficient transport of therapeutic agents across biological barriers, such as the skin, BBB and cellular membranes, overcoming challenges associated with traditional delivery methods/systems. The present chapter explores the fundamental principles of acoustic-based drug delivery, focusing on mechanisms such as cavitation, acoustic streaming and thermal effects. Additionally, it delves into advancements in microbubble and nanocarrier technologies, which enhance drug encapsulation and release at targeted sites with minimal off-target effects. Applications of these systems were highlighted in various diseases, emphasising their potential to improve therapeutic efficacy and patient outcomes. Despite the promising potential, challenges such as standardisation, scalability and long-term safety remain areas for further exploration. This chapter aims to provide a comprehensive overview of the science, technology and clinical applications of acoustic-based drug delivery, underscoring its role in revolutionising personalised medicine and advancing the frontier of drug delivery systems.