In the twenty-first century, microneedles based drug delivery is drawing attention worldwide in the research due to current signs of progress in the controlled release drug delivery through microneedles. The microneedles represent a promising technology to deliver therapeutic compounds into the skin for chronic complications like osteoporosis, diabetes, cancer and induction of immune responses from protein and DNA vaccines. However, the delivery of hydrophilic drugs and macromolecular agents are challenging. In this write up authors included the meticulous illustration of the chronological development of fabrication of microneedles with respect to an assortment of techniques, their modifications, clinical trials and regulatory perspectives period of 2000-2019. This review summarizes characterization, fabrications, biological applications and challenges. Additionally, relevant patents based on microneedle from USPTO) database are also highlighted.