Abstract: OBJECTIVE  The purpose of this research was to develop a self-assembled micelle using biocompatible copolymers Pluronic F127 (F127) and Vitamin E d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) to enhance the oral bioavailability and anti-cancer efficiency of honokiol (HK). METHODS  The optimized prescription honokiol micelle (HK-M) was prepared by an ethanol solvent evaporation method. HK-M was characterized by transmission electron microscopy(TEM) and HPLC. The dialysis bag method was used to assesse the cumulative amount of HK released from the HK-M. Caco-2 cells were applied to measure the permeability of HK-M. The bioavailability and in vivo anti-tumor effect were also evaluated. RESULTS  At the ratio of 4∶1 (F127∶TPGS), the HK-M was transparent and colourless with a small size (23.28 ± 2.01)nm and a spherical shape. The apparent solubility of HK in HK-M was dramatically increased to 4.76 mg/mL, suggesting that HK-M had good stability. Furthermore, encapsulation in micelles led to a sustained release of HK. HK-M enhances HK's permeability across Caco-2 cell monolayer. Compared with free HK, there was a 1.17-fold increase in the relative oral bioavailability for HK-M. Moreover, HK-M achieved a higher inhibition rate on tumor volume (35.17%) than HK group (14.86%). CONCLUSION