Background Driving the conventional drug in new applications has emerged as a research hotspot for disease treatment. Metformin (MET) is conventionally used for the treatment of type II diabetes. It has also been found to be a versatile molecule with wide biological functions, such as losing weight. anti-aging and anticancer activity. Rational design of nanoparticulate drug delivery systems (nano-DDS) could significantly improve drug delivery efficiency. Recently, a wide range of nano-DDS has been developed to improve the delivery efficacy of MET or to perform as versatile nanoplatforms for efficient drug delivery. Area covered In this review, we outline the emerging trends in advanced nano-DDS of MET, focusing on nano-DDS of MET for diabetes therapy, nano-DDS of MET for anticancer therapeutics, and nano-DDS of MET for other therapeutic aims. Expert opinion Despite the great progression in nano-DDS of MET, there's still a long way to truly put the conventional drug in new applications. Several important issues should be fully taken into consideration, such the manufacturing cost and economic burdens for patients, the biocompatibility and long-term toxicity of carrier materials, scale-up preparation difficulties, as well as the species gap between human beings and animal models.