The efficacy of many useful drugs can be improved by carrying out certain pharmaceutical manipulations in delivery route e.g. by transdermal drug delivery system. However, excellent impervious nature of stratum corneum restricts both the type and number of drugs that can be delivered to the systemic circulation by this route. A popular approach for increasing the percutaneous permeation of drug is to incorporate penetration enhancers into the formulations. The use of synthetic chemical enhancers for enhancing the percutaneous permeation of drugs is decreasing due to their long term effects and potential systemic toxicity. Hence, the main objective of this study was to evaluate the influence of triterpene and steroidal saponins on percutaneous permeation of carvedilol and to understand the mechanism(s) responsible for this effect.