Polymeric nanofibers with their large surface area per unit mass, biocompatibility, easy fabrication and surface modification find extensive use as filters and scaffolds in several biomedical applications like precision drug delivery, tissue engineering, formation of reinforced composite molecules and sensors. Though most of these applications are in nascent stages of development, some are being used commercially. Several strategies have been employed for development of nanofibers, but electrospinning technique has been used widely to modify several polymers into nanofibers and is probably the only strategy with potential for large-scale commercial production. It is a versatile process and has the ability to fabricate several nanofiber assemblies by enhancing the performance and introducing variations conducive for specific applications. Organic, inorganic or hybrid nanofibers exhibit refined mechanical features for enhanced sustained release or for regulated release of loaded drugs, which facilitates the application of nanofibers in precise delivery of drugs. This chapter provides a succinct account of the progress in preparation, performance and application of several nanofibers as drug delivery carriers for anti-inflammatory, antimicrobial, antitumor, cardiovascular, gastrointestinal and palliative therapies, emphasizing role of electrospinning process in the above applications.