The oral bioavailability of curcuminoids in healthy humans is markedly enhanced by micellar solubilisation but not further improved by simultaneous ingestion of sesamin, ferulic acid, naringenin and xanthohumol

Abstract

Available online A B S T R A C TCurcuminoids (curcumin, demethoxycurcumin and bis-demethoxycurcumin) are poorly absorbed and rapidly metabolised and excreted. We investigated in healthy young and aged women and men if co-administration of adjuvants (sesamin, ferulic acid, naringenin, and xanthohumol) alone or in combination with micellar solubilisation improves the bioavailability of curcuminoids. A single oral dose of 98 mg curcuminoids was administered as native curcuminoids (NC), native curcuminoids plus phytochemicals (NCP), curcuminoid micelles (MC) or curcuminoid plus phytochemical micelles (MCP). Total curcuminoids were quantified in blood samples collected over 24 h. Based on the area under the curve, NCP, MC, and MCP increased the bioavailability of the major curcuminoid curcumin 8-, 88-, and 73-fold, respectively, compared to NC. No sex or age differences were observed. Thus, simultaneous ingestion of phytochemicals does modestly increase curcuminoid bioavailability, but does not enhance the large increase in bioavailability observed with micellar curcuminoids.

Intratumoral Concentrations and Effects of Orally Administered Micellar Curcuminoids in Glioblastoma Patients

“…The administration of solid lipid curcumin particle formulations in osteosarcoma patients at doses of 4 g/ day resulted in maximum curcumin plasma concentrations of 41 ng/ml (28), which is fivefold lower than those reported here. The micellar curcumin formulation used in the present study, which was already shown to have superior oral bioavailability in humans over other formulations (18,19), should therefore be the formulation of choice for future studies.…”

“…To overcome this pharmacokinetic deficit, a number of strategies have been employed to increase the water solubility, physical stability, and intestinal permeability of curcumin. These strategies include ingestion in combination with other foods, formulation as micronized powders, combination with additional phytochemicals, and the development of controlled-release and nano-formulations (17)(18)(19).…”

Highly bioavailable micellar curcuminoids accumulate in blood, are safe and do not reduce blood lipids and inflammation markers in moderately hyperlipidemic individuals

“…Native curcuminoids have poor oral bioavailability , which may explain why previous human studies testing native curcuminoids have led to variable results. We hypothesize that curcuminoids with improved bioavailability will lower plasma lipids and inflammation in subjects at risk for the metabolic syndrome.…”

Enhanced absorption and pharmacokinetics of fresh turmeric (Curcuma Longa L) derived curcuminoids in comparison with the standard curcumin from dried rhizomes

“…Measurement of curcuminoids levels in plasma after administration of fresh turmeric juice powder was carried out by a standardized HPLC-DAD-ESI-MS/ MS procedure and the pharmacokinetic parameters were deducted from the plasma curcumin concentration-time plot as reported earlier (Cuomo et al, 2011;Krishnakumar et al, 2012). The relative absorption of curcumin from FTC in comparison with the standard curcumin DTC, was expressed in terms of the area under curve (AUC), since it is regarded as the most reliable method of expressing the absorption unlike the maximum plasma concentration of the drug (Cmax) which is just a single time point measurement (Kocher, Schiborr, Behnam, & Frank, 2015). Range and linearity for curcumin extracted from plasma was confirmed by spiking the standard curcumin and the internal standard, salbutamol.…”