Nobiletin is the most prevalent polymethoxyflavones existing in the citrus peels, and has demonstrated numerous health benefits, such as anti-inflammation, anti-cancer, anti-virus, and anti-diabetes. The oral bioavailability of nobiletin is limited due to its highly crystalline structure and poor water solubility. In this study, lecithin-based emulsion was developed with high loading of nobiletin (1%). The nobiletin-loaded emulsion was characterized by particle size, zeta potential, and rheological measurement. Through the in vitro model-TNO’s gastrointestinal model (TIM-1), the bioaccessibility of nobiletin was enhanced by emulsion as compared to oil suspension. Furthermore, the bioavailability and biotransformation of nobiletin were assessed using rat model through oral and intravenous administration. The Tmax and Cmax of nobiletin in the plasma were about 1h and 0.54±0.09μg/ml for oil suspension delivery, and 6h and 1.31±0.38μg/ml for emulsion delivery. Based on the calculation of area under the curves (AUC), the bioavailability of nobiletin delivered by emulsion was about 49%, which was nearly 2.2 times of that delivered by oil suspension. The analysis of plasma metabolites demonstrated that 4’-demethylated nobiletin had the highest concentration in the profile of demethylated metabolites. Moreover, the AUC of 4’-demethylated nobiletin delivered by emulsion was higher than that by oil suspension. Comparing the biotransformation kinetics between oral and intravenous administration, the reabsorption from the colon also played an important role for the overall bioavailability of nobiletin.

Assessment of oral bioavailability and biotransformation of nobiletin emulsion using <i>in vitro</i> and <i>in vivo</i> model

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

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Assessment of oral bioavailability and biotransformation of nobiletin emulsion using in vitro and in vivo model