The development of innovative approaches to deliver medications has been increasing, generating a growing interest in the dermatopharmaceutical field. For many therapies, transdermal drug administration in particular continues to be an appealing alternative method. It has advantages over traditional drug administration methods, which have drawn attention to them in recent years. Percutaneous medication administration is troublesome because the skin acts as a natural barrier and has a low penetration rate. Vesicular systems like liposomes, niosomes, elastic liposomes like ethosomes, and transferosomes have all been utilized to improve the transdermal dispersion of bioactives. Transferosomes seem to be a potential alternative among these. Hydrophilic actives, bigger molecules, peptides, proteins, and nucleic acids are few of the therapies that can be successfully delivered transdermally through transferosomes. The flexible structure for regulating capabilities and higher surface hydrophilicity to improve the solubility of transferosomes play a critical role in the transport of drugs and other solutes using hydration gradients, which act as a driving force to deliver the molecules into the skin. This results in increased overall permeation and controlled release of the drug into the skin layers. Transferosomes are said to have a number of applications, like the delivery of vaccines, proteins, anti-diabetic and anti-cancer drugs, anesthetics, and herbal drugs. They also have better patient compliance, improved bioavailability, and site-specific delivery and can serve as an emerging tool for transdermal delivery of almost all drugs and bioactives. This review provides an overview of the recent and relevant literature describing the emerging and versatile transformation of transferosomes in pharmaceutical research.