Over the years, scientists have been continually striving to develop innovative solutions to design and fabricate medicines with improved therapeutic potential. Conventional dosage forms, such as tablets, capsules, and injections, are limited when exploited for advanced therapeutics, such as drug targeting. To cater to these limitations, nanofibres have emerged as novel nanomaterials to provide enhanced bioavailability, targeted drug release, extended drug release profile, minimum toxicity, and reduced dosage frequency, which has indisputably improved patient adherence and compliance. This review will concern understanding the potential of drug-loaded nanofibres in drug delivery while comprehending a detailed description of their different production methods. The literature has been thoroughly reviewed to appreciate their potential in developing nanofibrous-based pharmaceutical formulations. Overall, this review has highlighted the importance, versatility, and adaptability of nanofibres in developing medicines with varied drug release kinetics. Several problems must be resolved for their full commercial realisation, such as the drug loading, the initial burst effect, the residual organic solvent, the stability of active agents, and the combined usage of new or existing biocompatible polymers.