The substantial impact of nanotechnology on material sciences is exemplified through zinc oxide nanomaterials (ZnO NMs), which play a pivotal role in healthcare and environmental applications. This comprehensive review focuses on the eco‐friendly synthesis of ZnO NMs and their cutting‐edge practices in biomedical, including drug delivery, bioimaging, and anticancer therapies. Exploring environmentally responsible production techniques for ZnO NMs aims to mitigate risks associated with conventional methods, such as the use of costly and toxic precursors. In addition, these green methodologies present opportunities for generating diverse and significant morphologies. The study delves into the inhibitory effects of these NMs against microbes, cancer, and inflammation. The utilization of ZnO NMs in disease treatment and diagnosis prompts us to explore recent developments in emerging biomedical applications. Leveraging ZnO variable optical characteristics, biodegradability, inherent biocompatibility, adaptable surface chemistry, and high stability, the review covers a range of remarkable research studies for novel applications that possibly open up the potential for identifying, treating, and preventing serious human diseases.