Assessment of Oral Bioavailability and Biotransformation of Emulsified Nobiletin Using and Models.

Nobiletin has received much attention for its promising biological activities. Owing to its limited solubility, various encapsulation strategies have been developed to enhance nobiletin bioavailability. However, the understanding of the bioavailability and biotransformation of nobiletin and the correlation between and data remains limited. This study developed a high-loading nobiletin (1%) emulsion. The models, which combined pH-stat lipolysis with a Franz cell, showed very good correlation with data for the relative bioavailability. Rat studies showed that nobiletin had a high absolute bioavailability (≈20% for oil suspension). Besides, the emulsification improved the amount of bioavailable nobiletin and its major metabolite in the blood by about two times, as compared to an oil suspension. This work provides scientific insights into a rapid screening method for delivery systems and a better understanding of the biological fate of nobiletin .