Mangiferin, a naturally occurring C-glucosylxanthone derived from various parts of the mango tree (Mangifera indica), has gained significant attention for its diverse pharmacological properties, including antioxidant, anti-inflammatory, antimicrobial, anticancer, and anti-diabetic activities. This mini-review provides an updated overview of the phytochemistry, pharmacokinetics, and medicinal properties of mangiferin. However, the low solubility (0.111 mg/mL) and oral bioavailability (less than 2%) of mangiferin pose significant challenges for its clinical application. To address these issues, the development of nanoformulations such as nanoparticles, micelles, and liposomes has been explored, which was proven to improve mangiferin's solubility, stability, and targeted delivery. These nanocarriers enhance the bioavailability and therapeutic efficacy of mangiferin, making it a promising candidate for various therapeutic applications. The review ends with the discussion of the safety of mangiferin and its formulations in addition to the potential for clinical translation.