Azadirachta indica, also known as neem, has been gaining interest in the era of modern-day medicine, owing to its extensive applications in homeopathic, Ayurvedic, and Unani medicine. This nature's drug store has long been investigated for its medicinal benefits, since all parts of this tree including leaves, seed, flower and bark have the potential to prevent numerous chronic diseases such as cancer, neurodegenerative disorders, cardiovascular disease, reproduction-related pathologies, as well as diabetes. Approximately 140 phytochemicals have been extracted from different parts of neem for pharmaceutical and agricultural applications. Among these bioactives, the active ingredient; neem leaf glycoprotein (NLGP) is currently gaining most interest, primarily due to its immunomodulatory properties. However, these therapeutic ingredients of neem get readily degraded when exposed to ultraviolet radiation. Encapsulation of these functional ingredients in novel nanocarriers ensures not only improvement in stability and sustainability, but also provides its controlled release, thus making it an ideal drug-delivery tool. This chapter focuses on providing stellar therapeutic potential of neem phytoconstituents, especially as an anticancer agent, while accentuating variegated promising strategies using various nanocarriers.