Mangiferin (MGF), a bioactive compound found in mangoes and their byproducts, possesses various pharmacological activities and holds potential for use in natural nutritional supplements and pharmaceuticals. However, the low solubility and poor bioavailability significantly limit its effectiveness. To address these limitations, this study employed the natural sweetener rebaudioside A (Reb A) to encapsulate MGF within self-assembled nanomicelle (SAM), resulting in the formation of nanoscale spherical particles with an encapsulation efficiency of 87.14% ± 0.56% and a drug loading capacity of 44.31% ± 0.28%. MGF-Reb A SAM improved both the water solubility and thermal stability of MGF through structural transformation from the crystalline to the amorphous form. Additionally, MGF-Reb A SAM exhibited sustained-release properties, with 92.32% of the MGF released within 12 h. The release kinetics followed a first-order model. In Caco-2 cell studies, MGF-Reb A SAM demonstrated good cellular compatibility and increased MGF permeability across intestinal epithelial cells by enhancing passive diffusion, thereby improving bioavailability. Pharmacokinetic analysis revealed that MGF-Reb A SAM increased the bioavailability of MGF 2.41-fold. In conclusion, the Reb A-based delivery system developed in this study enhances the physicochemical properties of MGF, offering a promising strategy for its future use in food supplements and pharmaceuticals.
Keywords: mangiferin; pharmacokinetics; rebaudioside A; self-assembled nanomicelles.