The convergence of nanotechnology and cancer therapeutics has opened new frontiers in the development of advanced drug delivery systems. Among the various nanocarriers, nanobubbles offer significant potential due to their unique properties, such as high payload capacity, responsiveness to external stimuli like ultrasound, and enhanced permeability and retention (EPR) effects. Functionalizing these nanobubbles with chitosan, a naturally derived biopolymer known for its biocompatibility, biodegradability, and ability to enhance cellular uptake, further improves their therapeutic efficacy. This review provides a comprehensive analysis of the synthesis, functionalization, and application of chitosan-functionalized nanobubbles in cancer therapy. We discuss their mechanism of action, including targeted drug delivery, ultrasound-mediated release, and immune modulation, alongside recent advancements and challenges in their clinical translation. This review also explores future directions in this rapidly evolving field, aiming to offer insights into the development of next-generation cancer therapeutics.