Abstract: Due to the effect of cuticle barrier, the transdermal penetration efficiency of most drugs is low. Therefore, the application of transdermal drug delivery system is greatly limited. Microneedle drug delivery system and nanodelivery system are the two most widely studied transdermal drug delivery systems. The microneedle drug delivery system can form tiny channels on the surface of the skin to promote drug penetration, and can quickly send nanodrugs to the capillaries to participate in the systemic circulation without touching the nerves in the dermis to cause pain. The nanodelivery system not only enhances drug penetration, but also improves the pharmacokinetic and pharmacodynamic properties of drugs, thereby increasing bioavailability, while minimizing adverse reactions. As a novel transdermal drug delivery carrier, microneedle-mediated nanodelivery system has shown great potential and promising prospect, attracting widespread attention in recent research.