Comparative absorption of curcumin formulations

Nutrition Journal

Jacob M Wilson¹  Martin Purpura²  Jordan M Joy¹  Allison V Calvanese¹  Ryan P Lowery¹  Ralf Jäger² 

[1]Department of Health Sciences and Human Performance, The University of Tampa, Tampa, FL 33606, USA

[2]Increnovo LLC, 2138 E Lafayette Pl, Milwaukee, WI 53202, USA

关键词: Bioavailability;    Absorption;    Curcumin;   

Others  :  801828
DOI  :  10.1186/1475-2891-13-11

 received in 2013-10-26, accepted in 2014-01-20,  发布年份 2014

【 摘 要 】

Background

The potential health benefits of curcumin are limited by its poor solubility, low absorption from the gut, rapid metabolism and rapid systemic elimination. The purpose of this study was the comparative measurement of the increases in levels of curcuminoids (curcumin, demethoxycurcumin, bisdemethoxycurcumin) and the metabolite tetrahydrocurcumin after oral administration of three different curcumin formulations in comparison to unformulated standard.

Methods

The relative absorption of a curcumin phytosome formulation (CP), a formulation with volatile oils of turmeric rhizome (CTR) and a formulation of curcumin with a combination of hydrophilic carrier, cellulosic derivatives and natural antioxidants (CHC) in comparison to a standardized curcumin mixture (CS) was investigated in a randomized, double-blind, crossover human study in healthy volunteers. Samples were analyzed by HPLC-MS/MS.

Results

Total curcuminoids appearance in the blood was 1.3-fold higher for CTR and 7.9-fold higher for CP in comparison to unformulated CS. CHC showed a 45.9-fold higher absorption over CS and significantly improved absorption over CP (5.8-fold) and CTR (34.9-fold, all p < 0.001).

Conclusion

A formulation of curcumin with a combination of hydrophilic carrier, cellulosic derivatives and natural antioxidants significantly increases curcuminoid appearance in the blood in comparison to unformulated standard curcumin CS, CTR and CP.

【 授权许可】

   
2014 Jäger et al.; licensee BioMed Central Ltd.

【 图 表 】

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【 参考文献 】

• [1]Chen A, Xu J, Johnson AC: Curcumin inhibits human colon cancer cell growth by suppressing gene expression of epidermal growth factor receptor through reducing the activity of the transcription factor Egr-1. Oncogene 2006, 25(2):278-287.
• [2]Bhattacharyya S, Mandal D, Sen GS, Pal S, Banerjee S, Lahiry L, Finke JH, Tannenbaum CS, Das T, Sa G: Tumor-induced oxidative stress perturbs nuclear factor-kappaB activity-augmenting tumor necrosis factor-alpha-mediated T-cell death: protection by curcumin. Cancer Res 2007, 67(1):362-370.
• [3]Jagetia GC, Aggarwal BB: “Spicing up” of the immune system by curcumin. J Clin Immunol 2007, 27(1):19-35.
• [4]DiSilvestro RA, Joseph E, Zhao S, Bomser J: Diverse effects of a low dose supplement of lipidated curcumin in healthy middle aged people. Nutr J 2012, 11:79. BioMed Central Full Text
• [5]Ringman JM, Frautschy SA, Cole GM, Masterman DL, Cummings JL: A potential role of the curry spice curcumin in Alzheimer’s disease. Curr Alzheimer Res 2005, 2:131-136.
• [6]Chuengsamarn S, Rattanamongkolgul S, Luechapudiporn R, Phisalaphong C, Jirawatnotai S: Curcumin extract for prevention of type 2 diabetes. Diabetes Care 2012, 35(11):2121-2127.
• [7]Chandran B, Goel A: A randomized, pilot study to assess the efficacy and safety of curcumin in patients with active rheumatoid arthritis. Phytother Res 2012, 26(11):1719-1725.
• [8]Ali T, Shakir F, Morton J: Curcumin and inflammatory bowel disease: biological mechanisms and clinical implication. Digestion 2012, 85(4):249-255.
• [9]Anand P, Kunnumakkara AB, Newman RA, Aggarwal BB: Bioavailability of curcumin: problems and promises. Mol Pharm 2007, 4(6):807-818.
• [10]Akazawa N, Choi Y, Miyaki A, Tanabe Y, Sugawara J, Ajisaka R, Maeda S: Curcumin ingestion and exercise training improve vascular endothelial function in postmenopausal women. Nutr Res 2012, 32(10):795-799.
• [11]Sugawara J, Akazawa N, Miyaki A, Choi Y, Tanabe Y, Imai T, Maeda S: Effect of endurance exercise training and curcumin intake on central arterial hemodynamics in postmenopausal women: pilot study. Am J Hypertens 2012, 25(6):651-656.
• [12]Joe B, Vijaykumar M, Lokesh BR: Biological properties of curcumin-cellular and molecular mechanisms of action. Crit Rev Food Sci Nutr 2004, 44(2):97-111.
• [13]Shishodia S, Sethi G, Aggarwal BB: Curcumin: getting back to the roots. Ann N Y Acad Sci 2005, 1056:206-217.
• [14]Ataie A, Sabetkasaei M, Haghparast A, Moghaddam A, Kazeminejad B: Neuroprotective effects of the polyphenolic antioxidant agent, Curcumin, against homocysteine-induced cognitive impairment and oxidative stress in the rat. Pharmacol Biochem Behav 2010, 96:378-385.
• [15]Naik S, Thakare V, Patil S: Protective effect of curcumin on experimentally induced inflammation, hepatotoxicity and cardiotoxicity in rats: evidence of its antioxidant property. Exp Toxicol Pathol 2011, 63:419-431.
• [16]Li S, Yuan W, Deng G, Wang P, Yang P, Aggarwal BB: Chemical composition and product quality control of turmeric (Curcuma longa L.). Pharmaceutical Crops 2011, 2:28-54.
• [17]Wahlström B, Blennow G: A study on the fate of curcumin in the rat. Acta Pharmacol Toxicol (Copenh) 1978, 43:86-92.
• [18]Vareed SK, Kakarala M, Ruffin MT, Crowell JA, Normolle DP, Djuric Z, Brenner DE: Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects. Cancer Epidemiol Biomarkers Prev 2008, 17:1411-1417.
• [19]Hassaninasab A, Hashimoto Y, Tomita-Yokotani K, Kobayashi M: Discovery of the curcumin metabolic pathway involving a unique enzyme in an intestinal microorganism. Proc Natl Acad Sci U S A 2011, 108:6615-6620.
• [20]Yallapu MM, Jaggi M, Chauhan SC: Curcumin nanoformulations: a future nanomedicine for cancer. Drug Discov Today 2012, 17(1-2):71-80.
• [21]Liu A, Lou H, Zhao L, Fan P: Validated LC/MS/MS assay for curcumin and tetrahydrocurcumin in rat plasma and application to pharmacokinetic study of phospholipid complex of curcumin. J Pharm Biomed Anal 2006, 40(3):720-727.
• [22]Yu H, Huang Q: Improving the oral bioavailability of curcumin using novel organogel-based nanoemulsions. J Agric Food Chem 2012, 60(21):5373-5379.
• [23]Hu L, Jia Y, Niu F, Jia Z, Yabg X, Jiao K: Preparation and enhancement of oral bioavailability of curcumin using microemulsions vehicle. J Agric Food Chem 2012, 60(29):7137-7141.
• [24]Khalil NM, Nascimento TC, Casa DM, Dalmolin LF, Mattos AC, Hoss I, Romano MA, Mainardes RM: Pharmacokinetics of curcumin-loaded PLGA and PLGA-PEG blend nanoparticles after oral administration in rats. Colloids Surf B: Biointerfaces 2013, 101:353-360.
• [25]Antony B, Merina B, Iyer VS, Judy N, Lennertz K, Joyal S: A pilot cross-over study to evaluate human oral bioavailability of BCM-95CG (Biocurcumax), a novel bioenhanced preparation of curcumin. Indian J Pharm Sci 2008, 70(4):445-449.
• [26]Cuomo J, Appendino G, Dern AS, Schneider E, McKinnon TP, Brown MJ, Togni S, Dixon BM: Comparative absorption of a standardized curcuminoid mixture and its lecithin formulation. J Nat Prod 2011, 74(4):664-669.
• [27]Sasaki H, Sunagawa Y, Takahashi K, Imaizumi A, Fukuda H, Hashimoto T, Wada H, Katanasaka Y, Kakeya H, Fujita M, Hasegawa K, Morimoto T: Innovative preparation of curcumin for improved oral bioavailability. Biol Pharm Bull 2011, 34(5):660-665.
• [28]Kulkarni SK, Akula KK, Deshpande J: Evaluation of antidepressant-like activity of novel water-soluble curcumin formulations and St. John’s wort in behavioral paradigms of despair. Pharmacology 2012, 89(1-2):83-90.
• [29]Lao CD, Ruffin MT, Normolle D, Heath DD, Murray SI, Bailey JM, Boggs ME, Crowell J, Rock CL, Brenner DE: Dose escalation of a curcuminoid formulation. BMC Complement Altern Med 2006, 6:10. BioMed Central Full Text
• [30]Jayaprakasha GK, Jaganmohan Rao L, Sakariah KK: Antioxidant activities of curcumin, demethoxycurcumin and bisdemethoxycurcumin. Food Chem 2006, 98(4):720-724.
• [31]Mahattanadul S, Panichayupakaranant P, Tungsinmonkong K: Comparison of the inhibitory potency of curcumin, demethoxycurcumin and bisdemethoxycurcumin on iNOS-derived NO in activated macrophages and on gastric ulcer in rats. Planta Med 2009, 75(9):J22.
• [32]Sandur SK, Pandey MK, Sung B, Ahn KS, Murakami A, Sethi G, Limtrakul P, Badmaev V, Aggarwal BB: Curcumin, demethoxycurcumin, bisdemethoxycurcumin, tetrahydrocurcumin and turmerones differentially regulate anti-inflammatory and anti-proliferative responses through a ROS-independent mechanism. Carcinogensis 2007, 28(8):1765-1773.
• [33]Osawa T, Sugiyama Y, Inayoshi M, Kawakishi S: Antioxidative activity of tetrahydrocurcuminoids. Biosci Biotechnol Biochem 1995, 59(9):1609-1612.
• [34]Mukhopadhyay A, Basu N, Ghata N, Gujral PK: Anti-inflammatory and irritant activities of curcumin analogues in rats. Agents Actions 1982, 12(4):508-515.