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Dextran sulfate (DXS) is a hydrophilic, non-toxic, biodegradable, biocompatible and safe biopolymer. These biomedically relevant characteristics make DXS a promising building block in the development of nanocarrier systems for several biomedical applications, including imaging and drug delivery. DXS polyanion can bind with metal oxide nanomaterials, biological receptors and therapeutic drug molecules. By taking advantage of these intriguing properties, DXS is used to functionalize or construct nanocarriers for specific applications. In particular, the diagnostic or therapeutic active agent-loaded DXS nanoparticles are prepared by simple coating, formation of polyelectrolyte complexes with other positively charged polymers or through self-assembly of amphiphilic DXS derivatives. These nanoparticles show a potential to localize the active agents at the pathological site and minimize undesired side effects. As DXS can recognize and be taken up by macrophage surface receptors, it is also used as a targeting ligand for drug delivery. Besides as a nanocarrier scaffold material, DXS has intrinsic therapeutic potential. DXS binds to thrombin, acts as an anticoagulant and exhibits an inhibitory effect against coagulation, retrovirus, scrapie virus and human immunodeficiency virus (HIV). Herein, biomedical applications involving the use of DXS as nanocarriers for drugs, biomolecules, and imaging agents have been reviewed. A special focus has been made on strategies used for loading and delivering of drugs and biomolecules meant for treating several diseases, including cancer, inflammatory diseases and ocular disease. [ABSTRACT FROM AUTHOR]