Skin has traditionally been used by various means to apply the medicaments for various purposes. Recent years have witnessed transdermal as a main route of delivery for various drugs which are difficult to deliver otherwise. Transdermal drug delivery offers several advantages mainly avoidance of first pass metabolism and gastric environment which would inactivate the drug. This review encompasses the basic anatomy of skin relevant to the transdermal route as a drug delivery and discuss in detail the various formulation strategies and permeation enhancement for better therapeutic effect. Finally, the review sumps up with the current technologies in the market and also discuss the future direction.