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Conducting polymers are an outstanding class of materials characterized by electroconducting properties that make them good candidates for applications in several sectors. Among them, polyaniline (PANI) is unique for its extraordinary ability to conduct electricity, biocompatibility and low toxicity. In spite of its surprising features, to date PANI have not yet found application in the practical uses, because of its low solubility and processability. In order to overcome these limitations, different approaches have been developed, such as polymer grafting processes, PANI-based composites and blends preparation. The present review describes the most recent advances on PANI applications in biomedical fields, such as antioxidant, antimicrobial and antivirus activity, drug delivery, cancer therapy, etc. A look to the synthetic procedures is also reported because it is crucial for the realization of more innovative materials in the next future.