Comparative Absorption of a Standardized Curcuminoid Mixture and Its Lecithin Formulation

• Published in: Journal of natural products (Washington, D.C.) Vol. 74; no. 4; pp. 664 - 669
• Main Authors: Cuomo, John, Appendino, Giovanni, Dern, Adam S, Schneider, Erik, McKinnon, Toni P, Brown, Mark J, Togni, Stefano, Dixon, Brian M
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society and American Society of Pharmacognosy 25.04.2011; Amer Chemical Soc; American Society of Pharmacognosy
• Subjects: Analysis; Biological and medical sciences; Chemistry, Medicinal; Chemistry, Pharmaceutical; Curcumin - analogs & derivatives; Curcumin - chemistry; Curcumin - pharmacokinetics; Curcumin - standards; Diarylheptanoids; General pharmacology; Humans; Lecithins - pharmacokinetics; Lecithins - standards; Life Sciences & Biomedicine; Medical sciences; Molecular Structure; Pharmacognosy. Homeopathy. Health food; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Plant Sciences; Reference Standards; Science & Technology; EFFICACY; BLACK PEPPER; INFLAMMATION; PIPERINE; DOWN-REGULATION; LIPOPOLYSACCHARIDE; OSTEOARTHRITIS; PHOSPHATIDYLCHOLINE; MAJOR CONSTITUENT; DEMETHOXYCURCUMIN; Human; Biological fluid; Healthy subject; Phospholipid; Complex lipid; Mixture; Property formulation relationship; Blood; Blood plasma; Organic pigment; Absorption; Dosage form; Phosphatidylcholine; Pharmacokinetics; Comparative study
• DOI: 10.1021/np1007262
• ISSN: 0163-3864; 1520-6025

The relative absorption of a standardized curcuminoid mixture and its corresponding lecithin formulation (Meriva) was investigated in a randomized, double-blind, crossover human study. Clinically validated dosages were used for both products, and plasma levels of all three major curcuminoids [curcumin (1a), demethoxycurcumin (1b), and bisdemethoxycurcumin (1c)] were evaluated. Total curcuminoid absorption was about 29-fold higher for Meriva than for its corresponding unformulated curcuminoid mixture, but only phase-2 metabolites could be detected, and plasma concentrations were still significantly lower than those required for the inhibition of most anti-inflammatory targets of curcumin. Remarkably, phospholipid formulation increased the absorption of demethoxylated curcuminoids much more than that of curcumin (1a), with significant differences in plasma curcuminoid profile between Meriva and its corresponding unformulated curcuminoid mixture. Thus, the major plasma curcuminoid after administration of Meriva was not curcumin (1a), but demethoxycurcumin (1b), a more potent analogue in many in vitro anti-inflammatory assays. The improved absorption, and possibly also a better plasma curcuminoid profile, might underlie the clinical efficacy of Meriva at doses significantly lower than unformulated curcuminoid mixtures.