Nanomedicine and nano-delivery systems hold unlimited potential in the developing sciences, where nanoscale carriers are employed to efficiently deliver therapeutic drugs at specifically targeted sites in a controlled manner, imparting several advantages concerning improved efficacy and minimizing adverse drug reactions. These nano-delivery systems target-oriented delivery of drugs with precision at several site-specific, with mild toxicity, prolonged circulation time, high solubility, and long retention time in the living system, which circumvent the problems associated with the conventional delivery approach. Recently, nanocarriers such as dendrimers, liposomes, nanotubes, and nanoparticles have been extensively investigated through structural characteristics, size manipulation, and selective diagnosis through disease imaging molecules, which are very effective and introduce a new paradigm shift in drugs. In this review, the use of nanomedicines in drug delivery has been demonstrated in treating various diseases with significant advances and applications in different fields. In addition, this review discusses the current challenges and future directions for research in these promising fields as well.