Transition-metal complexes have shown significant anti-tumour potential and have advanced towards clinical trials. However, tumour cells often develop resistance to chemotherapeutics, which couple to the inherent compound’s’ toxicity and solubility hampers their translation to the clinics. Therefore, besides the tremendous efforts to synthesise and characterise novel compounds, it is essential to create new drug delivery systems that circumvent these problems, allowing specific and selective delivery of drugs to tumour cells, thus decreasing the required dose and reducing side effects to the healthy tissue. Nano biotechnoloy has been providing for innovative solutions to address this challenge, via the smart design of nano formulations suitable for targeted delivery to the tumour microenvironment. In this review, we discuss recent nano systems combined with medicinal chemistry in cancer therapeutics, focusing on the clinical translation of such systems.