The skin covers a total surface area of approximately 1.8 m(2) and provides the contact between the human body and its external environment. Transdermal route of drug delivery has gained great interest in pharmaceutical research as it overcomes many problems associated with oral route of administration. Although the skin, particularly the stratum corneum presents a barrier to most drug absorption, it provides a large (1.2 m(2)) and accessible surface area for drug diffusion. Recently, various strategies have been used to augment the transdermal delivery of bioactives. Mainly, they include iontophoresis, electrophoresis, sonophoresis, chemical permeation enhancers, magnetophoresis, microneedles, vesicular systems (liposomes, niosomes, elastic liposomes such as ethosomes, transfersomes and transethosomes). Among these transethosomes appear to be more promising as they possess both lipophilic and hydrophilic regions and can accommodate drug molecules with wide range of solubility. Transethosomes can deform and pass through narrow constriction that is 5 to 10 times less than its own diameter. This high deformability gives better penetration of intact vesicles. These vesicles can be used for transdermal delivery of various classes of drugs like analgesics, anesthetics, corticosteroids, sex hormones, anticancer agents insulin etc.