Moringa oleifera leaf is a popular green leafy vegetable which has found its usefulness in the preparation of traditional stews and soups. Like most green leafy vegetable which are not around year‐round, the leaf is usually dried and pulverized for storage and easier handling, and despite the popularity of this processing technique, there is dearth of information on how drying affects the health‐promoting properties of the leaves. Hence, this study sought to investigate the effect of some drying methods (freeze‐drying, sun, air and oven drying) on the phytoconstituents, antioxidant properties, and biological activities of moringa leaf. This study revealed that drying methods significantly altered the phytoconstituents (phenolics, flavonoids, vitamin C, tannin, saponin, phytate, oxalate, alkaloid, cardenolides, and cardiac glycosides), antioxidant capacities (reducing power, Fe2+chelating, ABTS •+, DPPH, and • OH scavenging abilities), and enzyme inhibitory (α‐amylase and α‐glucosidase) effects of the leaf, with freeze‐drying being the most promising method for preserving the nutraceutical properties of moringa leaf. However, for practical application, the order of preference of the drying methods which ensures adequate retention of phytoconstituents and possibly biological activities of the leaf as observed in this study is freeze‐drying > air drying > sun drying > oven drying, in the order of decreasing magnitude.