Abstract
Curcumin exerts a wide range of beneficial physiological and pharmacological activities, including antioxidant, anti-amyloid, anti-inflammatory, anti-microbial, anti-neoplastic, immune-modulating, metabolism regulating, anti-depressant, neuroprotective and tissue protective effects. However, its poor solubility and poor absorption in the free form in the gastrointestinal tract and its rapid biotransformation to inactive metabolites greatly limit its utility as a health-promoting agent and dietary supplement. Recent advances in micro- and nano-formulations of curcumin with greatly enhanced absorption resulting in desirable blood levels of the active forms of curcumin now make it possible to address a wide range of potential applications, including pain management, and as tissue protective. Using these forms of highly bioavailable curcumin now enable a broad spectrum of appropriate studies to be conducted. This review discusses the formulations designed to enhance bioavailability, metabolism of curcumin, relationships between solubility and particle size relative to bioavailability, human pharmacokinetic studies involving formulated curcumin products, the widely used but inappropriate practice of hydrolyzing plasma samples for quantification of blood curcumin, current applications of curcumin and its metabolites and promising directions for health maintenance and applications.
Highlights
Curcumin is the major biologically active polyphenolic constituent in turmeric, called diferuloylmethane (1E,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,6-diene-3,5-dione)
This review, as compared to other curcumin-related reviews, summarizes the three broad formulation strategies that have been employed to enhance absorption and bioavailability, providing specific examples for each category. It reviews and contrasts the human pharmacokinetic studies that have been conducted with various formulations, and discusses the issues inherent in the majority of studies regarding the use of enzymatic hydrolysis of plasma samples prior to extraction and analysis
32-glycerides (Gelucire® ) and polysorbate 20 (BioCurc® ) [15]; fenugreek-derived galactomannan fiber (CurQfen® ) [28]; liquid droplets containing Gelucire® and caprylocaproyl polyoxyglycerides (Labrasol® ), a BioCurc® formulation [29]; colloidal dispersions using ghatti gum and glycerin (Theracurmin® ) [30,31,32,33]; a matrix of glycerol esters of fatty acids, medium chain triglycerides, hydroxymethylcellulose and sodium alginate (MicroActive Curcumin®) [34]; a proprietary mixture of surfactants, polar lipids and solvents (HydroCurc® ) [35]; solid lipid curcumin particles composed of docosahexaenoic acid (DHA), soy lecithin, stearic acid and vitamin C esters (Longvida® ) [36]; a blend of sodium caseinate and Tween 20 [37]; proprietary microcapsules (CurcushineTM); and a complex with acacia gum, quillaia and sunflower oil (TurmiPure® )
Summary
Curcumin is the major biologically active polyphenolic constituent in turmeric, called diferuloylmethane (1E,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,6-diene-3,5-dione) This review, as compared to other curcumin-related reviews, summarizes the three broad formulation strategies that have been employed to enhance absorption and bioavailability, providing specific examples for each category. It reviews and contrasts the human pharmacokinetic studies that have been conducted with various formulations, and discusses the issues inherent in the majority of studies regarding the use of enzymatic hydrolysis of plasma samples prior to extraction and analysis. In this review, formulated curcumin products that provide >100-fold better absorption than unformulated curcumin are considered highly bioavailable
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