Metallodrugs, which contain metal ions as active components, exhibit promising therapeutic effects compared to conventional organic drugs. This review explores various classes of metallodrugs, including platinum-, gold-, and ruthenium-based compounds, and their biomedical applications in treating cancer, bacterial, and inflammatory diseases. Despite their advantages, metallodrugs face challenges such as toxicity, selectivity, cost, and stability issues. Nanotechnology offers innovative solutions by enhancing drug delivery, stability, and bioavailability while reducing toxicity. Lipid-based, polymer-based, and inorganic nanoparticles serve as nanocarriers that enable targeted and controlled drug release in response to stimuli such as pH, temperature, and light. The paper further discusses preclinical and clinical challenges, including scalability and safety concerns, and presents future directions focusing on eco-friendly synthesis and improved therapeutic performance. Overall, nanotechnology represents a transformative approach for advancing metallodrug efficiency, offering precise, safe, and sustainable drug delivery systems for modern medicine.