Effect of curcumin-micelles adopting vitamin E-TPGS and Solutol HS 15 as carriers on solubility and oral bioavailability of curcumin / 中草药

ABSTRACT

Objective: To prepare curcumin-micelles adopting vitamin E-TPGS (VE-TPGS) and Solutol HS15 (SHS15) as carriers, and study the effect on solubility and oral bioavailability of curcumin (Cur). Methods: Cur was loaded into micelles between VE-TPGS and SHS15 by thin film dispersion method. Particle size, loading efficiency, entrapment efficiency, and in vitro release were carried on to estimate the influence of micelles on Cur; Moreover, oral bioavailability in rats was also evaluated. Results: The particle size was (35.79 ± 1.23) nm with polydispersity index (PDI) of 0.12 ± 0.03 when the optimized micelles ratio was at 3:7 of VE-TPGS and SHS15, which increased the solubility of Cur to 2.03 mg/mL in water. The entrapment efficiency and drug loading were 90.03% and 9.34%, respectively. The in vitro release profile showed a sustained release property compared with that of Cur. In addition, the relative bioavailability of micelles (AUC0~∞) compared with that of Cur (AUC0~∞) was 303.5% (P < 0.01). Conclusion: The Cur-micelles combined use of VE-TPGS and SHS15 shows great potential clinical application.