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It is our honor and privilege to serve as the Guest Editors of the Special Edition on “Nanostructures for Therapeutic Applications” for the journal “Current Bioactive Compounds”. The past decade has witnessed an unprecedented growth in the area of nanotechnology. This in turn has provided valuable tools to understand the biological systems and processes at a much closer level than was previously possible. The combination of nanotechnology and biology has also led to the development of a new generation of therapeutic devices with high therapeutic efficacy. This is mainly due to their ability to precisely interact with the sub-microscopic structures of living cells. The aim of the special edition is to provide a state-of-the-art, comprehensive account of the recent advances towards developing nanostructures for four different therapeutic applications. The article by Peach et al. discusses the recent developments in the nanotechnological approaches for the treatment of cancer. The authors provide an overview of the passive, active and external tumor targeting strategies using nanoparticle (NP) delivery systems. The article by Freeman et al., overviews the recent developments in the nanofabrication processes for promoting musculoskeletal tissue regeneration. The article discusses the various nanostructures currently been developed to modulate musculoskeletal cell functions to promote regeneration. The article by Wang et al., highlights the various unique nanostructures capable of by-passing the blood-brain barrier, a feat difficult to achieve using conventional therapeutic strategies. Finally, the article by Neal et al., presents an overview of the applications of nanomedicine to promote cardiovascular tissue regeneration. The guest editors would like to express their sincere gratitude to the editorial board of the Current Bioactive Compounds for their support. We would also like to appreciate all the authors for their valuable contributions in making this special edition a success.