Login Register Cart 0
Generic placeholder image

Pharmaceutical Nanotechnology

Editor-in-Chief

ISSN (Print): 2211-7385
ISSN (Online): 2211-7393

Back
Journal Home About Journal Editorial Board Journal Insight Current Issue Volumes/Issues
Subscribe
Research Article

Enhanced Water Dispersibility of Curcumin Encapsulated in Alginate-Polysorbate 80 Nano Particles and Bioavailability in Healthy Human Volunteers

Author(s): Roopa Govindaraju, Roopa Karki, Jayanthi Chandrashekarappa*, Mukunthan Santhanam, Akshay K.K. Shankar, Hanumanthachar K. Joshi and Goli Divakar

Volume 7, Issue 1, 2019

Page: [39 - 56] Pages: 18

DOI: 10.2174/2211738507666190122121242

Abstract

Background: The turmeric (Curcuma longa) plant, a perennial herb of the ginger family, is an agronomic crop in the south and southeast tropical Asia. Turmeric an Indian yellow gold and universal spice is described in Ayurveda, an ancient treatise on longevity and quality life for the treatment of various inflammatory disorders. The oral bioavailability of curcumin is low due to poor aqueous solubility, alkaline instability and speedy elimination.

Objective: The present study is designed to prepare alginate polysorbate 80 nanoparticles to enhance aqueous solubility/dispersibility, hence bioavailability.

Method: Curcumin-loaded alginate - polysorbate 80 nanoparticles were prepared by ionotropic gelation technique.

Results: The optimized nano particles exhibited higher encapsulation efficiency (95%), particle size of 383 nm and Zeta potential of +200 mV. Formulations exhibited very low dissolution in Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF), but the major portion released in SCF which is attributed to the digestibility of alginate in Simulated Colonic Fluid (SCF) under the influence of colonic micro flora. FTIR and DSC observations revealed the successful entrapment of curcumin in alginate polysorbate-80 nanoparticles. The nanoparticles were more spherical, discrete and homogeneous. In healthy human volunteers, the oral bioavailability (AUC) of curcumin increased 5-fold after the consumption of curcumin nanosuspension compared to curcumin suspension. Maximum plasma concentration Cmax- 636 ± 122 ng/ml was observed at tmax- 2h for nanosuspension, whereas Cmax-87.7 ± 17.9ng/ml at tmax- 4h for suspension.

Conclusion: Curcumin-loaded alginate - polysorbate 80 nanoparticles prepared by ionotropic gelation method, successfully entrapped curcumin. Both curcumin suspension and curcumin nanosuspension were safe and well tolerated and may thus be useful in the prevention or treatment of various inflammatory diseases of mankind.

Keywords: Bioavailability, curcumin, ionotropic gelation, nanoparticles, polysorbate 80, sodium alginate.

« Previous Next »
Graphical Abstract

[1]
Tayyem RF, Heath D, Al-Delaimy WK, Rock CL. Curcumin content of turmeric and curry powders. Nutr Cancer 2006; 55(2): 126-31.
[2]
Gupta NK, Dixit VK. Development and evaluation of vesicular system for curcumin delivery. Arch Dermatol Res 2011; 303(2): 89-101.
[3]
Shishodia S, Sethi G, Aggarwal B. Curcumin: getting back to the roots. N Y Acad Sci 2005; 1056: 206-17.
[4]
Bisht S, Maitra A. Systemic delivery of curcumin: 21st century solutions for an ancient conundrum. Curr Drug Discov Technol 2009; 6(3): 192-9.
[5]
Anand P, Kunnumakkara AB, Newman RA, Aggarwal BB. Bioavailability of curcumin: problems and promises. Mol Pharm 2007; 4: 807-18.
[6]
Das R, Kasoju N, Bora U. Encapsulation of curcumin in alginate-chitosan-pluronic composite nanoparticles for delivery to cancer cells. Nanomed: Nanotechnol Biol Med 2010; 6(1): 153-60.
[7]
Aggarwal B, Harikumar K. Potential therapeutic effects of curcumin, the anti-inflammatory agent, against neurodegenerative, cardiovascular, pulmonary, metabolic, autoimmune and neoplastic diseases. Int J Biochem Cell Biol 2009; 41(1): 40-59.
[8]
Cui J, Yu B, Zhao Y. Enhancement of oral absorption of curcumin by self-micro Emulsifying drug delivery systems. Int J Pharm 2009; 371(1): 148-55.
[9]
Mourtas S, Canovi M, Zona C, Aurilia D, Niarakis A, La Ferla B. Curcumin decorated Nano liposomes with very high affinity for amyloid-beta1-42 peptide. Biomaterials 2011; 32(6): 1635-45.
[10]
Tiyaboonchai W, Tungpradit W, Plianbangchang P. Formulation and characterization of curcuminoids loaded solid lipid nanoparticles. Int J Pharm 2007; 337(1): 299-306.
[11]
Wang YJ, Pan MH, Cheng AL, et al. Stability of curcumin in buffer solutions and characterization of its degradation products. J Pharm Biomed Anal 1997; 15(12): 1867-6.
[12]
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. Mol Nutr Food Res 2014; 58: 516-27.
[13]
Wahlström B, Blennow G. A study on the fate of curcumin in the rat. Acta Pharmacol Toxicol 1978; 43(2): 86-92.
[14]
Motwani S, Chopra S, Talegaonkar S, Kohli K, Ahmad F, Khar R. Chitosan “sodium alginate nanoparticles as submicroscopic reservoirs for ocular delivery: formulation, optimization and in vitro characterisation. Eur J Pharm Biopharm 2007; 68: 513-25.
[15]
Margulis K, Srinivasan S, Ware M, Summers H, Godin B, Magdassi S. Active curcumin nanoparticles formed from a volatile microemulsion template. J Mater Chem B Mater 2014; 2(24): 3745.
[16]
Roopa G, Jayanthi C, Pankaj B, Roopa K, Hanumanthachar KJ, Divakar G. Fabrication of casein-chitosan microparticles of curcumin for controlled delivery physico-chemical characterization. Micro Nanosyst 2017; 9(2): 1-9.
[17]
Rabanel J, Faivre J, Paka G, Ramassamy C, Hildgen P, Banquy X. Effect of polymer architecture on curcumin encapsulation and release from PEGylated polymer nanoparticles. Toward a drug delivery Nano-platform to the CNS. Eur J Pharm Biopharm 2015; 96: 409-20.
[18]
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. J Funct Foods 2015; 14: 183-91.
[19]
Ramaswamy S, Kuppuswamy G, Dwarampudi LP, Kadiyala M, Menta L, Kannan E. Development and validation of simultaneous estimation method for curcumin and piperine by RP-UFLC. Pak J Pharm Sci 2014; 27(4): 901-6.
[20]
Rashmi NG, Gurupadayya BM. Development and validation of a RP-UFLC method for estimation of polyphenol (gallic acid) in anti diabetic poly herbal formulation. Am J Phytomed Clin Ther 2015; 3(1): 34-42.
[21]
Ji H, Tang J, Li M, Ren J, Zheng N, Wu L. Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin. Drug Deliv 2014; 23(2): 459-70.
[22]
Sarika P, James N, Kumar P, Raj D, Kumary T. Gum arabic-curcumin conjugate micelles with enhanced loading for curcumin delivery to hepatocarcinoma cells. Carb Polym 2015; 134: 167-74.
[23]
Suryani N, Hatidjah AH, Nur IA. Rahmanpiu, Nina, M. Preparation of curcumin nanoparticle by using reinforcement ionic gelation technique. AIP Conf Proc 2017; 1-7.
[24]
Saha S, Ramesh R. Nanotechnology for Controlled Drug Delivery System. Int J Chemtech Res 2015; 7(4): 616-28.
[25]
Guterres S, Alves M, Pohlman A. Polymeric nanoparticles, nanospheres and nanocapsules, for cutaneous applications. Drug Target Insights 2007; 2: 11.
[26]
Tripathi A, Gupta R, Saraf SA. PLGA nanoparticles of anti tubercular drug: drug loading and release studies of a water in-soluble drug. Int J Pharm Tech Res 2010; 2(3): 2116-23.
[27]
Mohan PRK, Sreelakshmi G, Muraleedharan CV, Joseph R. Water soluble complexes of curcumin with cyclodextrins: characterization by ftraman spectroscopy. Vib Spectrosc 2012; 62: 77-84.
[28]
Pan K, Zhong Q, Baek SJ. Enhanced dispersibility and bioactivity of curcumin by encapsulation in casein nanocapsules. J Agric Food Chem 2013; 61(25): 6036-43.
[29]
Yiming M, Coombes A. Designing colon-specific delivery systems for anticancer drug-loaded nanoparticles: An evaluation of alginate carriers. J Biomed Mater Res A 2013; 102(9): 3167-76.
[30]
Facchi S, Scariot D, Bueno P, et al. Preparation and cytotoxicity of N-modified chitosan nanoparticles applied in curcumin delivery. Int J Biol Macromol 2016; 87: 237-45.
[31]
Paul W, Sharma C. Synthesis and characterization of alginate coated zinc calcium phosphate nanoparticles for intestinal delivery of insulin. Process Biochem 2012; 47(5): 882-6.
[32]
Shoba G, Joy D, Joseph T, Majeed M, Rajendran R, Srinivas PS. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med 1998; 64(4): 353-6.
[33]
Sasaki H, Sunagawa Y, Takahashi K, et al. Innovative preparation of curcumin for improved oral bioavailability. Biol Pharm Bull 2011; 34(5): 660-5.
[34]
Antony B, Merina B, Iyer VS, Judy N, Lennertz K, Joyal S. A pilot cross-over study to evaluate human oral bioavailability of BCM-95®CG (Biocurcumax™) a novel bio-enhanced preparation of curcumin. Indian J Pharm Sci 2008; 70(4): 445-9.
[35]
Vareed SK, Kakarala M, Ruffin MT. Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects. Cancer Epidemiol Biomarkers Prev 2008; 17: 1411-7.
[36]
Pawar Y, Munjal B, Arora S, Karwa M, Kohli G, Paliwal J. Bioavailability of a lipidic formulation of curcumin in healthy human volunteers. Pharmaceutics 2012; 4(4): 517-30.

Rights & Permissions Print Cite
Article Metrics
28
6
© 2024 Bentham Science Publishers | Privacy Policy