Recent advancements in molecular pharmacology and a deepened understanding of disease mechanisms have emphasized the need to precisely target specific cells responsible for disease onset and progression to prevent side effects and minimize systemic exposure. Drug delivery (DD) involves the strategies, formulations, technologies, and procedures employed to transport a pharmaceutical substance within the body of both humans and animals to produce the intended therapeutic outcome. The most frequently used delivery methods include topical (applied to the skin), transmucosal (such as nasal, buccal, sublingual, vaginal, ocular, and rectal), and inhalation routes. Traditional dosage forms release the drug rapidly, which can lead to variations in blood drug levels depending on the form of dosage. Current drug delivery systems (DDS) leverage cutting-edge technology to expedite the delivery of drugs systemically to specific target sites, thereby maximizing therapeutic efficacy while minimizing unintended accumulation in the body. Consequently, they play a pivotal role in disease management and treatment. Modern DDS present distinct advantages over conventional delivery systems, owing to their superior performance, automation, precision, and effectiveness. Utilizing nanomaterials or small-scale devices with multifunctional components, these systems are characterized by biocompatibility, biodegradability, and high viscoelasticity, resulting in prolonged circulating half-lives. This chapter offers a comprehensive overview of drug delivery systems’ historical progression and technological evolution. It also delves into recent developments in DDS, their therapeutic applications, challenges in their use, and potential future improvements for enhanced performance and utilization.