Drug delivery systems perform to improve the drug's efficacy and heal the affected region. Electrospun nanofibers are strong drug carriers as a scaffold due to their high specific surface area, easy processing, lightweight material. Fibrous scaffolds encapsulating functional bioactive agents are important for drug delivery applications, and they show higher encapsulation efficiency and higher drug loading capacity than various types of carrier materials such as hydrogels, micro/nanobeads, films, conventional fibers, and sponges. In comparison to conventional electrospinning, bi-component electrospinning where drug loading does not occur largely on the surface of the polymer matrix, core-shell nanofibers showed delayed release and a decrease in burst release because the drug was loaded into the core layer. The purpose of this mini-review is to investigate the production and applications of the drug-loaded bi-component nanofibers in structure core-shell, side-by-side, hollow nanofibers, and also emulsion nanofibers using co-axial nozzles. Further, the parameters which influence of these electrospinning process, such as working conditions and polymer properties, as well as drug delivery profile of the resulting nanofibers, have been outlined briefly. The limited clinical studies on the nanofibers have been discussed. Eventually, perspectives on the problems, possibilities, and new approaches for electrospinning advancements have been presented, as well.