Innovative Preparation of Curcumin for Improved Oral Bioavailability

Abstract

Curcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione] is the active ingredient of turmeric, which has a long history of being consumed as a dietary spice.1) In addition, turmeric is widely used in traditional Indian medicine to treat biliary disorders, anorexia, cough, diabetic complications, hepatic disorders, rheumatism, and sinusitis.2) Extensive investigation over the past five decades has indicated that curcumin reduces blood cholesterol, prevents low-density lipoprotein oxidation, inhibits platelet aggregation, suppresses thrombosis and myocardial infarction, suppresses symptoms associated with type 2 diabetes, rheumatoid arthritis, multiple sclerosis, and Alzheimer's disease, inhibits human immunodeficiency virus (HIV) replication, enhances wound healing, protects against liver injury, increases bile secretion, protects from cataract formation, and protects against pulmonary toxicity and fibrosis.3-5) Evidence indicates that the divergent effects of curcumin are dependent on its pleiotropic molecular effects.In spite of these attractive properties of curcumin, information on the therapeutic efficiency of curcumin has been limited, partly due to its poor oral bioavailability. 6) Curcumin was found to be poorly soluble in water, the maximum solubility of which in aqueous buffer (pH 5.0) was reported to be as low as 11 ng/ml.7) The limited solubility of curcumin, as well as extensive systemic metabolism, could be responsible for the low bioavailability of curcumin after oral delivery. [8][9][10] In addition, curcumin in solution may be sensitive to UV light, and so marked photochemical degradation could occur under UV exposure, 11) leading to difficulty in its handling for clinical use.A number of efforts have been made to design a soluble formulation of curcumin, but no suitable delivery options have been found so far. We have developed an effective preparation of curcumin, a nano-particle colloidal dispersion, with improved oral bioavailability, and named it THER-ACURMIN. It has the following unique properties: 1) it is an effective preparation for new health care products (beverages, food, and supplements) which may be taken at a much lower dosage; 2) it is soluble in water, which is a must for an effective beverage product; 3) the preparation is highly stable in light (UV), and, therefore, can be put into transparent PET bottles; 4) it is heat-stable, including high temperature sterilization conditions; 5) the preparation has no unpleasant odor or taste.The main purpose of this study was to provide evidence to support the improved bioavailability and alcohol-toxicity-reducing effect of THERACURMIN through oral delivery. We evaluated the plasma pharmacokinetics of this new curcumin preparation and compared the results with curcumin powder after oral administration in rats and healthy human subjects. We also investigated the effect of THERACURMIN on the toxicity of alcohol following drinking. MATERIALS AND METHODS Preparation of Curcumin Powder and THERACUR-MINCurcumin powder was extracted...

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

“…Theracurmin showed the highest Cmax and AUC among the 3 curcumin preparations in this study. Theracurmin was developed using a submicron-particle and surface-controlled drug-delivery system (22). Theracurmin has a high dispersibility, low aggregability, and high solubility in water and exhibits an over 30-fold higher bioavailability than conventional curcumin in rats and humans.…”

“…Theracurmin was supplied by the Theravalues Corporation (Tokyo, Japan) (22). The 2 other commercial preparations containing curcumin were obtained from stores: BCM-95 was from Life Extension Foundation and Meriva was from Thorne Research Inc.…”

“…Blood sample preparation and the measurement of plasma curcumin levels were previously reported (22,30). Briefl y, each plasma sample was incubated with 0.1 M sodium acetate buffer (pH 5.0) containing 1,000 U ␤-glucuronidase (Wako Pure Chemical Industries, Ltd., Japan) at 37˚C for 1 h to hydrolyze the curcumin conjugates.…”

“…Another lecithinized formulation of curcumin, Meriva, was tested in healthy volunteers, and found to improve absorption to about a 29-fold higher level than corresponding normal curcumin (21). Theracurmin, curcumin dispersed with colloidal submicron-particles, demonstrated oral bioavailability nearly 30 times higher than that of curcumin powder in both rats and humans (22,23).…”

Bioavailability Studies of BioTurmin-WD (Water Dispersible Curcuminoids) Using Caco-2 Cell Model

“…The yellow pigment of turmeric is being consumed as a dietary spice since ancient times and is a major ingredient of curry powders in India. Research on turmeric indicated that curcumin inhibits platelet aggregation, reduces blood cholesterol, suppresses symptoms associated with type 2 diabetes, and prevents low density lipoprotein oxidation and rheumatoid arthritis (Sasaki et al, 2011;Belcaro et al, 2010). In addition, curcumin has been reported to exhibit antibacterial, antioxidant and antimicrobial activities (Gupta, Patchva, & Aggarwal, 2013).…”