Electrospraying has emerged as a versatile technique in the pharmaceutical field due to its potential in drug delivery and formulation. With its advantages of cost‐effectiveness, reproducibility, ease of operation, and scalability, electrospraying offers numerous benefits for pharmaceutical applications. Notably, the production of nanoparticles using electrospraying provides unique properties, including small size, drug encapsulation capabilities, biocompatibility, and scalability. Electrospray nanoparticles have demonstrated significant promise in various drug delivery routes, such as oral and topical administration. These nanoparticles enhance drug stability, protection, and permeability, effectively overcoming limitations associated with these routes. Moreover, electrospray nanoparticles have proven valuable in targeted drug delivery, improving drug bioavailability and efficacy. Their ability to penetrate tissues and cells enables enhanced drug delivery to specific sites within the body. Additionally, electrospray nanoparticles can be tailored with targeting ligands or responsive components for controlled release and combination therapy, exhibiting successful applications in cancer treatment and neurological disorders. Therefore, electrospray nanoparticle technology shows great promise in biomedical applications, offering a versatile platform for targeted drug delivery and therapeutic interventions. This comprehensive review examines the various drug delivery applications of electrospraying and provides insights into its possibilities and challenges. The paper discusses the principles, methods, and parameters of electrospraying, while also exploring its use in fabricating drug delivery systems, addressing poorly soluble drugs. By synthesizing the findings from multiple studies, this review offers a comprehensive understanding of electrospraying's current state and potential in the pharmaceutical industry.