Abstract
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.
Highlights
Curcumin, a major active constituent found in Curcuma sp., is classified in group 4 of BCS (Biopharmaceutical Class System) [1]
To demonstrate the beneficial approach on the tocopherol polyethylene glycol succinate (TPGS)-curcumin nanoparticle, we studied the pharmacokinetic profile after oral administration and its effectiveness to treat ulcerative colitis model after the rectal route
This report describes the development of the TPGS-stabilized curcumin nanoparticle with a detail study to demonstrate the beneficial application of nanotechnology as well as the presence of TPGS to improve the therapeutic value of curcumin, a BCS 4 active compound
Summary
A major active constituent found in Curcuma sp., is classified in group 4 of BCS (Biopharmaceutical Class System) [1]. This means solubility is a key factor when determining the absorption. Low permeability is a second contribution for its low bioavailability after oral administration. Pharmaceutics 2017, 9, 24 was found out to be 2.55 ± 0.02 106 cm/s, ruling out the role of efflux pathways in the low oral bioavailability of curcumin. In addition to poor solubility and permeability, the low bioavailability of curcumin is worsened by intensive hepatic metabolism to more hydrophilic substances which are inactive [2].
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