Hyaluronan (HA), a multifunctional, high molecular weight glycosaminoglycan, is a component of the majority of extracellular matrices. HA is synthesised in a unique manner by a family of hyaluronan synthases, degraded by hyaluronidases and exerts a biological effect by binding to families of cellular receptors, the hyaladhedrins. Receptor binding activates signal pathways in endothelial cells leading to proliferation, migration and differentiation collectively termed angiogenesis. HA and associated enzymes are implicated in the aetiology of cardiovascular disease and cancer and manipulation of HA expression offers a therapeutic target. HA microspheres have been developed as drug delivery agents to deliver HA to sites of disease and also in diagnosis. In this review we discuss some of the recent therapeutic applications of hyaluronan in tissue repair, as a drug delivery system and the synthesis, application and delivery of hyaluronannanoparticles to target drugs to sites of disease.