Biopolymer Additives Enhance Tangeretin Bioavailability in Emulsion-Based Delivery Systems: An In Vitro and In Vivo Study

The oral bioavailability of tangeretin, a poly(methoxyflavone) found in citrus fruits, is typically very low because of its extremely limited solubility. In this research, tangeretin was encapsulated within whey protein-stabilized emulsions containing ingredients that may alter their behavior under gastrointestinal conditions and enhance the bioavailability of tangeretin after oral administration: cinnamaldehyde (CA), gum arabic (GA), or hydroxypropyl methylcellulose (HPMC). The presence of these ingredients altered the size, aggregation state, and encapsulation efficiency of tangeretin in the emulsions. In vitro studies demonstrated that the bioaccessibility of the encapsulated tangeretin was much higher than that of a crude tangeretin oil suspension. Particularly, the addition of HPMC increased the bioaccessibility of tangeretin from around 36 to 90%. In vivo pharmacokinetics results using rats indicated that tangeretin concentration in the plasma increased from 4- to 20-fold after encapsulation, especially in the presence of HPMC. HPMC also prolonged the release of tangeretin to 22 h. Tangeretin preferentially accumulated within the liver and kidney of the animals. Overall, the knowledge confirmed that structured emulsion-based delivery systems could be used to improve the oral bioavailability of hydrophobic functional ingredients.