Tangeretin (5,6,7,8,4'-pentamethoxyflavone) is a polymethoxylated flavonone that can be found predominantly in the peel of citrus fruits. Tangeretin has been documented to have many bio-functionalities, which include anti-inflammatory, anti-proliferative, and anti-carcinogenesis properties. However, due to the structurally substituted methoxy group on the 15-carbon benzo-?-pyrone skeleton backbone, tangeretin is hydrophobic and exhibits poor bioavailability when ingested orally. In the present study, an optimized emulsion-based system was formulated for tangeretin oral delivery. In this optimized emulsion system, the encapsulated tangeretin was mixed with homogenously entrapped tangeretin crystal and exhibited remarkable storage stability over six months. In vitro lipolysis and gastrointestinal model (TIM-1) revealed that emulsion delivered tangeretin was digested considerably faster and more bioaccessible than unformulated suspension. In vivo pharmacokinetic study on mice again confirmed that the oral bioavailability of tangeretin was significantly improved by emulsion-based system. Moreover, tangeretin in the emulsion system was more effective to inhibit growth and development of colorectal cancer while not inducing serious toxicity effect. This novel approach using emulsion formulation can also be used for future development of hydrophobic bioactive compounds with high loading and long term storage stability.

Effect of emulsion-based delivery system on the orally ingested tangeretin: Bioavailability, efficacy, and toxicity

248th National Meeting (2014)

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