Applying nanobubbles (NBs) for contrast-enhanced ultrasound imaging has received increased attention. NBs are biocompatible, multifunctional, theranostic agents. Their properties of high echogenicity and stability create an agent suitable for ultrasonography diagnosis. Their favorable properties of size, in vivo stability, and ease of modification are being exploited to implement a theranostic platform for cancer treatment. The considerable development offers the potential to overcome drug resistance and adverse side effects that are associated with traditional chemotherapy. This review outlines the principles of ultrasonography and angiogenesis. Microbubbles and micelles are also discussed to underline the superior capabilities of NBs for the application. NBs could passively accumulate to tumor tissue by enhanced permeability and retention effect. In addition, it can also achieve the active transportation by surface modification. Active targeting modalities and stimuli-responsive drug delivery modifications generate a therapeutic vehicle. The cytotoxicity of NBs formulations, multimodal imaging capability, active targeting mechanisms, and drug delivery methods are highlighted to confirm the NB as a vehicle for targeted treatment and enhanced ultrasound imaging.