Novel Drug Delivery System (NDDS) is providing an exceptional improvement in terms of safety, efficacy & quality of conventional drug therapy. Skin is the largest organ present in the body and provides the most convenient route of administration. Transdermal Drug Delivery System (TDDS) is one of the methods introduced under NDDS for providing systemic effect in the body through skin. Although the innovation proves to have maximum patient compliance, it holds limited bioavailability due to the presence of Stratum Corneum, a chief protective skin barrier. A lot of novel advanced transdermal technologies in the form of Penetration Enhancers have been developed to increase bioavailability. This review would discuss the active approaches involved for facilitating drug permeability. It includes renowned methods like Iontophoresis, Sonophoresis, Electroporation, Magnetophoresis, Photomechanical waves, and also other new technologies. This review further highlights certain products under transdermal technologies which are approved and currently in the market. We anticipate that in the future, the limitations of the physical approaches would be overcomed and new advancements along with combination techniques will be in the highlights, resulting in better patient compliance and efficient treatment. Keywords: drug delivery, novel system, ultrasonic waves, physical transdermal approaches, ultrasound.