Nanotechnology and nanoscience are relatively new technological endeavors that encompass the study, control, manipulation, and assembly of multifarious nanoscale components into materials, systems and devices to serve human interest and needs. Among the various currently used nanostructures for high technology applications polymeric nanofibers have received immense interest due to the ease of fabrication, controllable size/shape, and properties. Polymeric nanofibers have been extensively investigated for diversified applications, including filtration, barrier fabrics, wipes, personal care, biomedical, and pharmaceutical applications. This review mainly focuses on the fabrication of therapeutic agent loaded polymeric nanofibers and their controlled/sustained release behavior for the delivery of these active agents for various therapeutic applications. The nonwoven biodegradable polymeric nanofiber matrices are currently being reported as topical/local therapeutic agent delivery systems and as resorbable/biodegradable gauze for wound healing applications.