Transdermal drug delivery systems (TDDS) are used to deliver the drug(s) or the therapeutically active substances through topical route primarily through skin. Relatively very small numbers of drugs are administered transdermally because in many cases the physical properties of drugs, including polarity and molecular size, have limited its capacity to deliver the particular dug transdermally. Now a day’s transdermal drug delivery techniques are used in various therapeutic areas like motion sickness management, heart disease treatment, hormones replacement, management of pain and smoking cessation etc. TDDS increases the potency of drugs and decreases the relative side effects. We reviewed different approaches used to enhance the drug delivery transdermally (e.g., particulate and vesicle based method, modified stratum corneum method, electrically based method, vehicle interaction method, removed stratum corneum method). As the stratum corneum is the main barrier in transdermal drug delivery, so the approaches can also be classified in three main categories in order to circumventing the barriers related to stratum corneum only (based on drug vehicle, chemical enhancers, physical enhancers). Here we focused mainly on the microneedles (MNs) based approach for transdermal drug delivery.