Citrus aurantifoliais part of the Rutaceae family and belongs to the genus Citrus. It is widely used in food, the chemical industry, and pharmaceuticals because it has a unique flavor and odor. It is nutrient-rich and is beneficial as an antibacterial, anticancer, antioxidant, anti-inflammatory, and insecticide. Secondary metabolites present inC. aurantifoliaare what give rise to biological action. Flavonoids, terpenoids, phenolics, limonoids, alkaloids, and essential oils are among the secondary metabolites/phytochemicals discovered inC. aurantifolia. Every portion of the plant’sC. aurantifoliahas a different composition of secondary metabolites. Environmental conditions such as light and temperature affect the oxidative stability of the secondary metabolites fromC. aurantifolia. The oxidative stability has been increased by using microencapsulation. The advantages of microencapsulation are control of the release, solubilization, and protection of the bioactive component. Therefore, the chemical makeup and biological functions of the various plant components ofC. aurantifoliamust be investigated. The aim of this review is to discuss the bioactive components ofC. aurantifoliasuch as essential oils, flavonoids, terpenoids, phenolic, limonoids, and alkaloids obtained from different parts of the plants and their biological activities such as being antibacterial, antioxidant, anticancer, an insecticide, and anti-inflammatory. In addition, various extraction techniques of the compounds out of different parts of the plant matrix as well as the microencapsulation of the bioactive components in food are also provided.