This review article deals with latest literature studies on the potential use of polymer ultrathin and nanosized structures obtained by electrospinning to design novel engineered materials with bioactive properties. The electrofluidodynamic process offers the option to form high-performance bioactive systems based on polymer yarns of nanofibers or coatings of nanobeads with high surface-to-volume ratios. The electrospun and electrosprayed nanostructures can be further functionalized by encapsulation with bioactive fillers and substances. For both scenarios, the resultant polymer nanostructures present unique bioactive properties capable of providing a beneficial impact over human's health and with improved and advanced performance for biomedicine, pharmaceutics, nutrition, bioengineering, and healthcare applications. These novel functional materials attained by the electrospinning technology can be of interest for many bioactive applications such as functional food design, food packaging, functional coatings, controlled delivery of drug solutions and, mainly, tissue engineering. This article is purposely designed to gather, for the first time, most recent and promising multi-and inter-disciplinary develop-