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Penetration Enhancers have vast potential and if utilized thoroughly, can be beneficial route in the drug delivery. Penetration Enhancers facilitates the drug delivery in various ways. They are therefore also referred as sorption enhancers or accelerants. This review focusses on the various enhancement techniques which are widely used to increase the bioavailability of the drugs. This review explores the various penetration enhancers with their mechanism of action and their roles in enhancement techniques. One of the reasons why the Transdermal drug delivery has not been successful compared to other delivery system, is the impervious nature of the versatile skin. It has been reported that individual penetration enhancer are not able to bring that effect which is achieved by the combination of penetration enhancer or mixture of penetration enhancer. Different penetration enhancers act at different site of action and have different mechanism of action ranging from altering metabolic activity within the skin, or exerting an influence on the thermodynamic activity of the drug in its vehicle. The major limitation in transdermal drug delivery is the diffusion of drug molecules to cross, one of the most versatile barriers of skin. A number of skin penetrations enhancers have been investigated and explored for skin penetration enhancement. Further, developments and initiatives are required to evaluate the mechanism of enhancement techniques. A thorough understanding of this penetration enhancer has been discussed and future implications explored.