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Transdermal drug delivery is a viable and clinically proven route of administration. This route specifically requires overcoming the mechanical barrier provided by the Stratum Corneum of epidermis and vascular and nervous networks within the dermis. First-generation Transdermal patches and second-generation iontophoretic patches have been translated into commercial clinical products successfully. The current review reports different studies that aim to enhance the transdermal delivery of biopharmaceutical using microneedles and their effect on drug delivery. Microneedles (MN) are the micron-scale hybrid between transdermal patches and hypodermic syringes. Microneedles are tested and proven to show better delivery of the drugs, overcoming the drawbacks of hypodermic syringes. Multiple microneedles designs have been fabricated i.e. solid, coated, hollow, and polymer microneedles. Hollow microneedles are shorter in length but similar to hypodermic needles and have pore for infusion of liquid formulation of the drug. Solid microneedles a patch is applied after creating a hole in the skin; Drugs are coated on the surface of Coated microneedles; Polymer microneedles can be of different types like dissolving, non-dissolving or hydrogel-forming made up of polymers. Various advantages and limitations associated with the use of these techniques are discussed. Delivery of peptide and protein molecules with microneedles represents a significant opportunity for a better clinical outcome and hence value creation compared to standard injectable routes of administration. The advancement in various formulation and microfabrication techniques are currently being focused to aid the delivery of protein drugs via microneedles. The most recent advances and limitations in Microneedles -mediated protein and peptide delivery were discussed., (© 2021. Controlled Release Society.)