Abstract: Orthodontic treatment typically requires an extended duration of 1-2 years to complete the treatment. Accelerating the rate of tooth movement during orthodontic treatment is essential for shortening the overall treatment duration. After the completion of orthodontic treatment, a prominent concern arises in the form of orthodontic relapse, where the teeth tend to revert to their original positions. This issue affects approximately 60% of the global population, underscoring the importance of implementing effective measures to address orthodontic relapse. An approach in this regard involves the targeted administration of herbal and synthetic drugs applied directly to the specific area of interest to facilitate tooth movement and prevent orthodontic relapse. Apart from this, researchers are investigating the feasibility of utilizing different types of nanoparticles to improve the process of orthodontic tooth movement. In recent years, there has been a noticeable increase in the number of studies examining the effects of various drugs on orthodontics. However, the currently available literature does not provide significant evidence relating to orthodontic tooth movement. In this review, the authors provide valuable information about the drugs and nanomaterials that are capable of further enhancing the rate of orthodontic tooth movement and reducing the risk of orthodontic relapse. However, a notable hurdle remains, i.e., there is no marketed formulation available that can enhance orthodontic tooth movement and reduce treatment time. Therefore, researchers should try herbal-synthetic approaches to achieve a synergistic effect that can enhance orthodontic tooth movement. In this nutshell, there is an urgent need to develop a non-invasive, patient-compliant, and cost-effective formulation that will provide quality treatment and ultimately reduce the treatment time. Another critical issue is orthodontic relapse, which can be addressed by employing drugs that slow down osteoclastogenesis, thereby preventing tooth movement after treatment. Nevertheless, extensive research is still required to overcome this challenge in the future.