The prospective route of using Citrus reticulata peel biowaste as a powerful source for creating antiepileptic therapies is examined in this book chapter. A sustainable and financially feasible way to treat the urgent global health problem of epilepsy is via the huge amounts of peel waste produced by the quantity of citrus fruits that are produced globally. The chemical makeup of citrus reticulata peels is explored in detail in this chapter, with a focus on the bioactive substances that are present, including terpenes, flavonoids, and essential oils found to have neuroprotective qualities. To clarify these citrus-derived chemicals’ methods of action on neuronal pathways and ion channels linked to epileptic activity, the discussion steers through the experimental data supporting their antiepileptic potential. This book chapter emphasizes the significance of sustainable practices in pharmaceutical development by providing insights into the extraction methods and formulation approaches for using these bioactive chemicals for medicinal applications. Moreover, the chapter examines preclinical and clinical research supporting the safety and effectiveness of Citrus Reticulata peel extracts in the treatment of epileptic seizures. This article provides a thorough overview of potential treatment pathways by examining the possible synergistic effects of mixing citrus bioactive with traditional antiepileptic medications. This chapter ends by recommending that natural chemicals from Citrus Reticulata peels that are generated from biowaste be included in mainstream research and development for antiepileptic drugs. This chapter aims to make way for novel and sustainable methods of managing epilepsy by promoting a greater comprehension of the molecular processes and clinical consequences.