In many clinical applications, the transdermal route is used as an alternative approach to avoid significant limitations associated with oral drug delivery. There is a long history for drug delivery through the skin utilizing transdermal microneedle arrays. Microneedles are reported to be highly efficient and versatile devices. This technique has attracted scientific and industrial interests, due to its outstanding characteristics such as painless penetration, excellent medicinal efficiency, relative protection and affordability. The microneedles have shown considerable potential to create advanced functional devices with remarkable properties for biomedical applications such as delivery of very large substances with ionic and hydrophilic physicochemical properties. In this review we present a summary of recent advances in microneedles-based drug delivery, typical materials used for their construction and fabrication methods that improves the delivery of critical substances through the protective membranes. Further, it explores the practicality of innovative microneedles used as a drug delivery tool. Microneedles are emerging tools that have shown profound potential for biomedical applications. Transdermal microneedle technologies are likely to become a preferred route of therapeutic substances administration in the future since they are effective, painless, and affordable.