Elevated plasma sugar is the foremost metabolic disorder around the globe, with an alarmingly rising mortality rate, and it exacerbates the patient's pathological condition. Following a research review, India had the world's greatest incidence of diabetes in 2000, with 31.7 million cases. Around 2030, the WHO forecasts that the global prevalence of diabetic instances might double. Multiple conventional hypoglycemic medications are adequate, yet they have a multitude of unpleasant side effects. Under the inclusion of numerous constituents in a plant with fewer negative impacts on peripheral organs, herbal novel formulations exhibit excellent synergistic efficacy. This study emphasizes on the biochemical constituents of medicinal herbs that inhibit Dipeptidyl peptidase-4 (DPP-4) enzymes which reduce blood glucose levels. The field of nanotechnology has an affordable price point and a higher safeguarding profile. The biosynthesis of herbal metal nanoparticles is one of the most promising approaches, with an outstanding pharmacokinetic profile, enhanced penetrability, and an environmentally friendly formulation. There are currently a handful of novel herbal formulations accessible on the market for sale. Regarding this, the authors of the present study investigated the molecular pharmacokinetic and pharmacodynamic profile status of medicinal herbs in numerous preclinical and clinical trials in future developments for their utility in treating this serious illness.