<p>Transferosomes are innovative lipid-based vesicles that have garnered significant attention as pioneering drug delivery systems for transdermal administration. These highly flexible and deformable vesicles comprise phospholipids and edge activators, such as ethanol or terpenes, which enable them to penetrate the stratum corneum barrier and deliver a wide range of therapeutic agents, including proteins, peptides, and various medications. This review discusses the composition, mechanism of action, and transformative role of transferosomes in transdermal drug delivery, focusing on their diverse formulations and characterization techniques. The composition of transferosomes, including the effect of phospholipids, solvents, and edge activators, plays a crucial role in determining their properties and efficacy. Various methods, such as thin-film hydration, reverse-phase evaporation, and freeze–thawing, have been employed to prepare transferosomes, and characterization techniques, such as vesicle size, zeta potential, and entrapment efficiency, are essential for optimizing their performance. The applications of transferosomes in delivering antioxidants, anticancer drugs, corticosteroids, anti-inflammatory agents, and herbal compounds are discussed, highlighting their potential to enhance drug bioavailability, reduce side effects, and improve patient compliance. Despite the challenges associated with stability and high production costs, transferosomes offer a promising solution for effective and versatile drug delivery through the skin. Further advancements in technology and formulation techniques are expected to address these challenges and pave the way for the widespread use of transferosomes in personalized medicine and targeted drug delivery.</p>