Background: Drug delivery of phytochemicals has gained interest recently due to their remarkable
health effects. Apigenin, a plant flavonoid, has antioxidant, anti-inflammatory and anticancer
activities but its delivery is challenging. It could be absorbed through the whole intestine, however, it
has poor bioavailability due to its low aqueous solubility. In Europe, the daily intake was estimated to
be as low as 3 ± 1 mg. Pellets offer several advantages such as improved bioavailability and various resultant
drug release profiles can be obtained by simply mixing pellets with different coatings.
Objective: The objective of our study was to develop a carrier system containing 20 mg apigenin thus
enhancing intake and to offer reduction of oxidative stress which can cause inflammation in the intestine.
Method: The apigenin powder was dispersed in aqueous solution of binding material and layered onto
the inert cores in a fluidized bed apparatus. The layered cores were further coated with enteric polymers
and the process parameters were optimized.
Results: The prepared pellets met with the requirements and have good physical characteristic. 10%
(w/w) Eudragit® L was suitable for enteric coating with a complete release at pH 6.8 within 1 hour. 15%
(w/w) Eudragit® FS coating ensured acid resistance ability and colonic delivery. The therapeutic efficiency
was confirmed with antioxidant activity measurement by using DPPH* assay.
Conclusion: Enteric coated spheres allow targeted delivery into the intestine and colon thus reaching
the main absorption site. Pellets were proved to be an optimal delivery system for apigenin thus providing
enhanced apigenin intake.