Plant-derived drugs or formulations have always been explored because of their lesser side effects and toxicities compared to synthetic drugs and they have been widely used as traditional and complementary medicines for the management of many diseases including cancer. The major challenges faced were the absorption of the plantderived drugs, their stability, bioavailability, and transport to the intended sites inside the body. Recent progress in nanotechnology has helped to minimize these limitations and hence phyto-nanoformulations are slowly growing in preclinical trials as well as clinical use. The use of various nanostructures such as nano-micelles, lipid nanoparticles, carbon nanotubes, polymer nanoparticles, and nanoliposomes and various types of drug delivery vehicles such as polybutylcyanoacrylate, polylactic-c- -glycolic acid, and lactoferrin has immensely helped in increasing the effectiveness of phytochemical drugs by increasing their stability, better pharmacokinetics and reducing the toxicity and side effects. Phyto-nanoformulations having natural product components such as curcumin, piperine, quercetin, berberine, scutellarin, baicalin, stevioside, silybin, gymnemic acid, naringenin, capsicum oleoresin, emodin, and resveratrol have been shown to improve the condition of patients diagnosed with diseases such as neurodegenerative disorders, diabetes, infections, and cancer. Phyto nanoformulations can also be used to treat disorders of the brain where the blood-brain barrier is impervious to the drugs. These phyto-nanoformulations have been shown to target several molecular cell-signaling and metabolic pathways. This chapter covers the compositions of phyto-nanoformulations and how they have been used to control several diseases.