Extensive research has been conducted on ZrO2 nanostructures due to their favorable biocompatibility, low toxicity, and promising prospects in various biomedical applications. They can be used as drug carriers, facilitating the administration of therapeutic substances into the body while enhancing their effectiveness and safety. This is achieved by regulating the timing, location, and rate at which drugs are released within the body. Several factors can influence the effectiveness of drug loading onto ZrO2 nanostructures, such as the physicochemical characteristics of the drugs, the surface properties of the ZrO2 nanostructures, and the specific methods used for drug loading. A wide range of drugs may be loaded onto ZrO2 nanostructures including anti-cancer drugs, antibiotics, anti-inflammatory drugs, antifungal drugs, anti-osteoporotic drugs, etc. The release kinetics of drugs can be influenced by different factors, such as the size and shape of ZrO2 nanostructures, the pH and temperature of the release medium, and the characteristics and molecular weight of the specific drug being released. While ZrO2 nanostructures have demonstrated significant potential as drug delivery systems, further research on these structures is essential to optimize drug loading and release strategies.