Dose-escalation and pharmacokinetic study of nanoparticle curcumin, a potential anticancer agent with improved bioavailability, in healthy human volunteers

Abstract

THERACURMIN can safely increase plasma curcumin levels in a dose-dependent manner at least up to 210 mg without saturating the absorption system. To the best of our knowledge, THERACURMIN is the first nanoparticle formulation of curcumin that demonstrates improved bioavailability in human subjects. We believe this compound could be a promising tool when testing the potential anticancer effects of curcumin in clinical trials.

Colloidal Submicron-Particle Curcumin Exhibits High Absorption Efficiency—A Double-Blind, 3-Way Crossover Study—

“…The total curcumin content in each preparation was considered to be approximately equal without breaking the capsules. Theracurmin was reported to be used at 100-400 mg in patients with cancer or healthy elderly volunteers for chronic treatment in clinical studies, indicating that at least 400 mg of Theracurmin was safe (24)(25)(26)(27). Moreover, more than 10 phase 2 clinical trials are now ongoing using 180 mg of Theracurmin, and no signifi cant adverse effect has been reported so far.…”

“…After normalization, AUC 0-24h and Cmax were signifi cantly higher with Theracurmin than with BCM-95 and Meriva. Although the plasma curcumin levels increased dependently with the intake dose, the correlation between plasma curcumin levels and intake doses of these forms of DDS curcumin was not linear in some clinical studies (21,25). Therefore, further pharmacokinetic studies are needed to clarify the possible effects of the oral doses on blood curcumin levels by adjusting the same intake doses of DDS curcumin or examining the effects of multiple doses.…”

“…This is because there is a possibility of the degradation of curcumin itself and disintegration of its micelles due to instability caused by destroying preparations in an attempt to standardize the amount. The dosage of each curcumin preparation was determined based on recommended amounts for commercial use and clinical studies (17,21,(24)(25)(26)(27)(28)(29). The clinical benefi ts were obtained at these doses.…”

“…Nine subjects were enrolled in this study; the cohort included 5 males (56%), the cohort included 5 males and 4 females, with a mean age of 25 (24)(25)(26)(27)(28)(29)(30)(31)(32) Fig. 1.…”

Dose escalation and pharmacokinetic study of nanoparticle curcumin… by Kanai et al., CCP 69:65–70, 2012

“…Kanai et al [1] report on the pharmacokinetic properties in healthy human volunteers of theracurmin, a novel nanoparticular formulation of the diet-derived putative cancer chemopreventive agent curcumin. The plasma concentrations reported in this paper are of curcumin conjugates, not of parent curcumin, because the authors routinely hydrolysed plasma samples prior to HPLC analysis using beta-glucuronidase.…”