The medicinal plant is well-regarded for its potential to combat several diseases. Phytochemicals acquired from these plants, such as terpenoids, flavonoids, and alkaloids, are utilized to treat a variety of disorders but have several drawbacks, such as low solubility and bioavailability. Nanotechnology is a crucial method to create a nanoformulation with active pharmaceutical ingredients from such phytochemicals, which are made at the nanodimensions, that is, 1–100 nm. Nanoformulations increase the stability, absorption efficiency, and targeted delivery of therapeutic compounds, which can enhance the efficacy of treatment of any disease. Nanoformulations have some enlightening features like improved bioavailability of biochemicals, increased solubility, targeted delivery, controlled release, and protection from degradation. This chapter gives a comprehensive insight into these natural resources implemented for various biomedical applications. It highlights the potential of different plant-based biochemicals to develop various nanomaterials. Bioactive-based nanomaterials are developed and characterized using various techniques and are discussed, which provide proper understanding of their significance, like production of antimicrobials as well as antioxidants. Nanomaterials obtained from these plants have various other applications in drug delivery, wound dressing, and increasing food shelf life, which indicates their various applications. Some nano-formulated plant-derived compounds, such as curcumin, resveratrol, and quercetin, possess inflammation-reducing potential and antioxidant activities. However, there are some challenges from such plant-based nanoformulations, like regulatory aspects, environmental implications, and economic susceptibility. This chapter will briefly elaborate on the clinical applications of plant-based nanomaterials.