Synthesis and application of nanostructured molybdenum disulphide particles and complex composites have been studied for several decades. They offer many attractive properties which are linked to the transition character of the base element, i.e. molybdenum, and high chemical activity of sulphur, an element of the oxygen family. Significant progress in our understanding of the processes involved in nucleation, growth, and shaping of molybdenum disulphide nanoparticles was achieved, and the mechanisms underlying their biological properties and catalytic activity were investigated; however, many questions remain. In this topical review, a number of representative examples are used to illustrate recent progress in nucleation and growth of various molybdenum disulphide nanostructures with the aim to provide a snapshot of the spectrum of practically important fabrication methods, from simplest solution-based techniques to the most advanced chemical vapour deposition and plasma-enhanced chemical vapour deposition techniques. We then review the most promising applications of these nanostructures in medicine, focusing on anti-cancer therapy, drug delivery and medical imaging, with the key advantages and opportunities presented by molybdenum disulphide nanoparticles and composites over other similar materials and nano-architectures. The outlook section focuses on present challenges in the synthesis, e.g. sophisticated control over particle structure and chemical activity, as well as advanced biomedical applications of molybdenum disulphide nano-structures, and proposes some strategies to overcome these challenges and problems.