Bioavailability of curcumin from a novel mouth dissolving lozenge

Sasikumar Menon; Mandar Mhatre; Manjusha Rajarshi; Jatin Thakkar

doi:10.18203/2319-2003.ijbcp20180674

Authors

Sasikumar Menon Institute for Advanced Training and Research in Interdisciplinary Sciences, Sion, Mumbai, Maharashtra, India
Mandar Mhatre Institute for Advanced Training and Research in Interdisciplinary Sciences, Sion, Mumbai, Maharashtra, India
Manjusha Rajarshi Consultant, Regulus Healthcare Summit, Mumbai, Maharashtra, India
Jatin Thakkar Managing Director, Gelnova Laboratories (I) Pvt. Ltd., Pawane, Navi Mumbai, Maharashtra, India

DOI:

https://doi.org/10.18203/2319-2003.ijbcp20180674

Keywords:

Bioavailability, Cucurmin lozenge, LC-MS/MS, Turmeric

Abstract

Background: Cucurmin is the main component of curcuminoids in turmeric (Curcuma longa). Turmeric, popularly used as food colourant, is traditionally used as a medicinal herb owing to its antioxidant, anti-inflammatory, antimicrobial and anticancer properties. The gastric absorption of curcumin is poor and therefore various forms like encapsulation in liposomes, polymeric nanoparticles, cyclodextrin encapsulation, lipid complexes, polymer-curcumin complex etc. have been evaluated.

Methods: In the current study, a novel lozenge of 100mg turmeric extract in mouth dissolving formulation is evaluated for bioavailability of curcumin as compared with the conventional hard gelatin capsule containing 475mg curcumin. Fourteen healthy male subjects of Indian origin are dosed in a two way, two treatments, two sequence cross-over balanced, randomized design. Blood samples are collected sequentially to cover the plasma concentration-time curve to obtain a reliable estimate of the extent of absorption. Blood plasma is processed and analyzed using a validated isocratic HPLC-MS/MS method to estimate the concentration of curcumin.

Results: Curcumin is detected at m/z 369à177, while the internal standard diazepam is detected as m/z 285à193 to quantify curcumin. Results indicate a significant increase in bioavailability of curcumin from the lozenge (C_max188.863±22.9620ng/ml; AUC_0-t 897.026±65.4844ng/mL*hr) as compared to the hard gelatin capsule (C_max 96.458±15.8272ng/ml; AUC_0-t 440.744±77.3470ng/ml*hr).

Conclusions: Mouth dissolving lozenge could be a pragmatic approach to circumvent the low bioavailability of curcumin from therapeutic formulations.

Metrics

Metrics Loading ...

Author Biography

Sasikumar Menon, Institute for Advanced Training and Research in Interdisciplinary Sciences, Sion, Mumbai, Maharashtra, India

References

Aggarwal BB, Kumar A, Bharti AC. Anticancer potential of curcumin: preclinical and clinical studies. Anticancer research. 2003 Jan 1;23(1/A):363-98.

Lestari ML, Indrayanto G. Curcumin. InProfiles of drug substances, excipients and related methodology 2014 Jan 1;39:113-204. Academic Press.

Anand P, Kunnumakkara AB, Newman RA, Aggarwal BB. Bioavailability of curcumin: problems and promises. Molecular pharmaceutics. 2007 Nov 14;4(6):807-18.

Rao EV, Sudheer P. Revisiting curcumin chemistry part I: A new strategy for the synthesis of curcuminoids. Indian journal of pharmaceutical sciences. 2011 May;73(3):262.

Manolova Y, Deneva V, Antonov L, Drakalska E, Momekova D, Lambov N. The effect of the water on the curcumin tautomerism: A quantitative approach. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy. 2014 Nov 11;132:815-20.

Mahady GB, Pendland SL, Yun G, Lu ZZ. Turmeric (Curcuma longa) and curcumin inhibit the growth of Helicobacter pylori, a group 1 carcinogen. Anticancer research. 2002;22(6C):4179-81.

Reddy RC, Vatsala PG, Keshamouni VG, Padmanaban G, Rangarajan PN. Curcumin for malaria therapy. Biochemical and biophysical research communications. 2005 Jan 14;326(2):472-4.

Vera‐Ramirez L, Pérez‐Lopez P, Varela‐Lopez A, Ramirez‐Tortosa M, Battino M, Quiles JL. Curcumin and liver disease. Biofactors. 2013 Jan 1;39(1):88-100.

E Wright L, B Frye J, Gorti B, N Timmermann B, L Funk J. Bioactivity of turmeric-derived curcuminoids and related metabolites in breast cancer. Current pharmaceutical design. 2013 Oct 1;19(34):6218-25.

Naksuriya O, Okonogi S, Schiffelers RM, Hennink WE. Curcumin nanoformulations: a review of pharmaceutical properties and preclinical studies and clinical data related to cancer treatment. Biomaterials. 2014 Mar 1;35(10):3365-83.

Kiuchi F, Goto Y, Sugimoto N, Akao N, Kondo K, Tsuda Y. Nematocidal activity of turmeric: synergistic action of curcuminoids. Chemical and Pharmaceutical Bulletin. 1993 Sep 15;41(9):1640-3.

Wright JS. Predicting the antioxidant activity of curcumin and curcuminoids. Journal of Molecular Structure: Theochem. 2002 Aug 30;591(1-3):207-17.

Priyadarsini KI, Maity DK, Naik GH, Kumar MS, Unnikrishnan MK, Satav JG, et al. Role of phenolic OH and methylene hydrogen on the free radical reactions and antioxidant activity of curcumin. Free Radical Biology and Medicine. 2003 Sep 1;35(5):475-84.

Iqbal M, Sharma SD, Okazaki Y, Fujisawa M, Okada S. Dietary supplementation of curcumin enhances antioxidant and phase II metabolizing enzymes in ddY male mice: possible role in protection against chemical carcinogenesis and toxicity. Basic & Clinical Pharmacology & Toxicology. 2003 Jan 1;92(1):33-8.

Aggarwal BB, Harikumar KB. Potential therapeutic effects of curcumin, the anti-inflammatory agent, against neurodegenerative, cardiovascular, pulmonary, metabolic, autoimmune and neoplastic diseases. The international journal of biochemistry & cell biology. 2009 Jan 1;41(1):40-59.

Basnet P, Skalko-Basnet N. Curcumin: an anti-inflammatory molecule from a curry spice on the path to cancer treatment. Molecules. 2011 Jun 3;16(6):4567-98.

Chandran B, Goel A. A randomized, pilot study to assess the efficacy and safety of curcumin in patients with active rheumatoid arthritis. Phytotherapy research. 2012 Nov 1;26(11):1719-25.

Kloesch B, Becker T, Dietersdorfer E, Kiener H, Steiner G. Anti-inflammatory and apoptotic effects of the polyphenol curcumin on human fibroblast-like synoviocytes. International immunopharmacology. 2013 Feb 1;15(2):400-5.

Pulido-Moran M, Moreno-Fernandez J, Ramirez-Tortosa C, Ramirez-Tortosa M. Curcumin and health. Molecules. 2016 Feb 25;21(3):264.

Schneider C, Gordon ON, Edwards RL, Luis PB. Degradation of curcumin: from mechanism to biological implications. Journal of agricultural and food chemistry. 2015 Apr 2;63(35):7606-14.

Sharma RA, Euden SA, Platton SL, Cooke DN, Shafayat A, Hewitt HR, et al. Phase I clinical trial of oral curcumin: biomarkers of systemic activity and compliance. Clinical Cancer Research. 2004 Oct 15;10(20):6847-54.

Ravindranath V, Chandrasekhara N. Metabolism of curcumn-studies with [3H] curcumin. Toxicology. 1981 Jan 1;22(4):337-44.

Pan MH, Huang TM, Lin JK. Biotransformation of curcumin through reduction and glucuronidation in mice. Drug metabolism and disposition. 1999 Apr 1;27(4):486-94.

Prasad S, Tyagi AK, Aggarwal BB. Recent developments in delivery, bioavailability, absorption and metabolism of curcumin: the golden pigment from golden spice. Cancer research and treatment: official journal of Korean Cancer Association. 2014 Jan;46(1):2.

Xie M, Fan D, Zhao Z, Li Z, Li G, Chen Y, et al. Nano-curcumin prepared via supercritical: Improved anti-bacterial, anti-oxidant and anti-cancer efficacy. International journal of pharmaceutics. 2015 Dec 30;496(2):732-40.

Maiti K, Mukherjee K, Gantait A, Saha BP, Mukherjee PK. Curcumin–phospholipid complex: preparation, therapeutic evaluation and pharmacokinetic study in rats. International journal of pharmaceutics. 2007 Feb 7;330(1-2):155-63.

Kocher A, Schiborr C, Behnam D, Frank J. 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. Journal of functional foods. 2015 Apr 1;14:183-91.

Chen W, Fan-Havard P, Yee LD, Cao Y, Stoner GD, Chan KK, et al. A liquid chromatography–tandem mass spectrometric method for quantification of curcumin-O-glucuronide and curcumin in human plasma. Journal of Chromatography B. 2012 Jul 1;900:89-93.

Hsieh YW, Huang CY, Yang SY, Peng YH, Yu CP, Chao PD, et al. Oral intake of curcumin markedly activated CYP 3A4: in vivo and ex-vivo studies. Scientific reports. 2014 Oct 10;4:6587.

Kurita T, Makino Y. Novel curcumin oral delivery systems. Anticancer research. 2013 Jul 1;33(7):2807-21.

Schiborr C, Kocher A, Behnam D, Jandasek J, Toelstede S, Frank J. The oral bioavailability of curcumin from micronized powder and liquid micelles is significantly increased in healthy humans and differs between sexes. Molecular Nutrition & Food Research. 2014 Mar 1;58(3):516-27.