This study was conducted to evaluate the potential benefit of particle reduction down to nanoscale on
curcumin, a unique natural active compound facing therapeutic problems due to low solubility and permeability. In addition, the presence of
TPGS as a
surfactant for multiple functions on
curcumin nanoparticle was addressed. Observation was focused on bioavailability enhancement after
oral administration and local anti-inflammatory improvement after rectal dosing. Nanonization of
curcumin was performed using an up-scalable top down method. Specific animal models were used to study the in vivo kinetic profile and the
biological activity of
curcumin nanoparticle, compared with
curcumin powder. d-α-
tocopherol polyethylene glycol 1000 succinate (
TPGS)-stabilized
curcumin nanoparticle was prepared through homogenization with high pressure of the 1500 bar. An in vivo study was performed after
oral administration of the preparations to male healthy Wistar rats, to monitor the plasma kinetic profile of
curcumin. The
biological activity study was conducted after
rectal administration of the preparations in Wistar rats induced by
2,4,6-trinitrobenzene sulfonic acid to develop
ulcerative colitis. The
curcumin nanoparticle with a size of approximately 200 nm was successfully produced and revealed a better in vivo kinetic profile over the larger size of
curcumin mixed with
TPGS, with bioavailability (AUC0-∞) that was accounted for seven-fold. In addition, the
TPGS-stabilized
curcumin nanoparticle demonstrated a superior local anti-inflammatory effect in
ulcerative colitis, indicated by the shifting of observed parameters close to the healthy status. The tremendously improved anti-inflammatory effect of the
TPGS-stabilized
curcumin nanoparticle was found with a very low dose. Reducing the particle size of
curcumin down to ~200 nm with the presence of
TPGS seems to be a promising approach to improving the therapeutic value of
curcumin.