Using in vitro and in vivo models to evaluate the oral bioavailability of nutraceuticals

Journal of Agricultural and Food Chemistry

Volumn 63, Issue 5, 2015, Pages 1332-1338

  Ting, Yuwen ^a   Zhao, Qin ^a   Xia, Chunxin ^a   Huang, Qingrong ^a  

^a RUTGERS UNIVERSITY   (United States)

Author keywords

bioaccessibility; bioavailability; Caco 2; in vitro digestion; lipolysis; metabolism; nutraceutical; pharmacokinetics; TIM 1

Indexed keywords

DIAGNOSIS; FORECASTING; METABOLISM; PHARMACOKINETICS;

BIOACCESSIBILITY; BIOAVAILABILITY; CACO-2; IN-VITRO DIGESTIONS; LIPOLYSIS; NUTRACEUTICALS; TIM-1;

BIOCHEMISTRY;

DRUG;

ANALYSIS; BIOAVAILABILITY; BIOLOGICAL MODEL; CACO 2 CELL LINE; DIET SUPPLEMENTATION; DIGESTION; HUMAN; IN VITRO STUDY; METABOLISM; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS;

ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; DIETARY SUPPLEMENTS; DIGESTION; HUMANS; IN VITRO TECHNIQUES; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS;

EID: 84922638187     PISSN: 00218561     EISSN: 15205118     Source Type: Journal    
DOI: 10.1021/jf5047464     Document Type: Review

References (71)

1. Tewfik, S.; Tewfik, I. Nutraceuticals, functional foods and botanical dietary supplements; promote wellbeing and underpin public health World Rev. Sci. Technol. Sustain. Dev. 2008, 5 (2) 104-123
2. Go, V. L. W.; Harris, D. M.; Srihari, P. In Global Overview of the Role of Nutraceuticals in Cancer; Sarkar, F. H., Ed.; Springer: Dordrecht, The Netherlands, 2012; pp 1-10.
3. Scheepens, A.; Tan, K.; Paxton, J. W. Improving the oral bioavailability of beneficial polyphenols through designed synergies Genes Nutr. 2010, 5 (1) 75-87
4. Scalbert, A.; Williamson, G. Dietary intake and bioavailability of polyphenols J. Nutr. 2000, 130 (8) 2073S-2085S
5. Ting, Y. W.; Li, S.; Ho, C.-T.; Huang, Q. Emulsion in oral delivery of bioactive lipophilic phytochemicals. In Nutrition, Functional and Sensory Properties of Foods; Ho, C.-T.; Mussinan, C.; Shahidi, F.; Colitis, E. T., Eds.; Royal Society of Chemistry: London, UK, 2013; Vol. 344, pp 231-242.
6. Ting, Y.; Jiang, Y.; Ho, C.-T.; Huang, Q. Common delivery systems for enhancing in vivo bioavailability and biological efficacy of nutraceuticals J. Funct. Food 2014, 7, 112-128
7. Zhu, Q. Y.; Zhang, A.; Tsang, D.; Huang, Y.; Chen, Z.-Y. Stability of green tea catechins J. Agric. Food Chem. 1997, 45 (12) 4624-4628
8. Zhu, Q. Y.; Holt, R. R.; Lazarus, S. A.; Ensunsa, J. L.; Hammerstone, J. F.; Schmitz, H. H.; Keen, C. L. Stability of the flavan-3-ols epicatechin and catechin and related dimeric procyanidins derived from cocoa J. Agric. Food Chem. 2002, 50 (6) 1700-1705
9. Wen, X.; Walle, T. Methylated flavonoids have greatly improved intestinal absorption and metabolic stability Drug Metab. Dispos. 2006, 34, 1786-1792
10. Wang, X. Y.; Wang, Y.-W.; Huang, Q. R., Enhancing stability and bioavailability of polyphenols using nanoemulsions. In Micro/Nano Encapsulation of Active Food Ingredients; Huang, Q. R.; Given, P.; Qian, M., Eds.; Oxford University Press: Oxford, UK, 2009; Vol. 1007.
11. Su, Y. L.; Leung, L. K.; Huang, Y.; Chen, Z. Y. Stability of tea theaflavins and catechins Food Chem. 2003, 83 (2) 189-195
12. McDougall, G. J.; Fyffe, S.; Dobson, P.; Stewart, D. Anthocyanins from red cabbage-stability to simulated gastrointestinal digestion Phytochemistry 2007, 68 (9) 1285-1294
13. Bermudez-Soto, M. J.; Tomas-Barberan, F. A.; Garcia-Conesa, M. T. Stability of polyphenols in chokeberry (Aronia melanocarpa) subjected to in vitro gastric and pancreatic digestion Food Chem. 2007, 102 (3) 865-874
14. Bell, L. N. Stability testing of utraceuticals and functional foods. In Handbook of Nutraceuticals and Functional Foods; Wildman, R. E. C., Ed.; CRC Press: New York, 2001; pp 501-516.
15. Yang, X.; Tian, H.; Ho, C.-T.; Huang, Q. Stability of citral in emulsions coated with cationic biopolymer layers J. Agric. Food Chem. 2011, 60 (1) 402-409
16. McClements, D. J.; Decker, E. A.; Park, Y.; Weiss, J. Designing food structure to control stability, digestion, release and absorption of lipophilic food components Food Biophys. 2008, 3 (2) 219-228
17. Kim, M. K.; Park, K. S.; Yeo, W. S.; Choo, H.; Chong, Y. In vitro solubility, stability and permeability of novel quercetin-amino acid conjugates Bioorg. Med. Chem. 2009, 17 (3) 1164-1171
18. Cohen, R.; Schwartz, B.; Peri, I.; Shimoni, E. Improving bioavailability and stability of genistein by complexation with high-amylose corn starch J. Agric. Food Chem. 2011, 59 (14) 7932-7938
19. Trevaskis, N. L.; Charman, W. N.; Porter, C. J. H. Lipid-based delivery systems and intestinal lymphatic drug transport: a mechanistic update Adv. Drug Deliver. Rev. 2008, 60 (6) 702-716
20. Porter, C. J. H.; Trevaskis, N. L.; Charman, W. N. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs Nat. Rev. Drug Discovery 2007, 6 (3) 231-248
21. Fricker, G.; Kromp, T.; Wendel, A.; Blume, A.; Zirkel, J.; Rebmann, H.; Setzer, C.; Quinkert, R. O.; Martin, F.; Muller-Goymann, C. Phospholipids and lipid-based formulations in oral drug delivery Pharm. Res. 2010, 27 (8) 1469-1486
22. McDougall, G. J.; Dobson, P.; Smith, P.; Blake, A.; Stewart, D. Assessing potential bioavailability of raspberry anthocyanins using an in vitro digestion system J. Agric. Food Chem. 2005, 53 (15) 5896-5904
23. McClements, D. J.; Li, Y. Review of in vitro digestion models for rapid screening of emulsion-based systems Food Funct. 2010, 1 (1) 32-59
24. Failla, M. L.; Huo, T.; Thakkar, S. K. In vitro screening of relative bioaccessibility of carotenoids from foods Asia Pac. J. Clin. Nutr. 2008, 17 (S1) 200-203
25. Ting, Y.; Jiang, Y.; Lan, Y.; Xia, C.; Lin, Z.; Roger, M. A.; Huang, Q. Use of viscoelastic emulsions to increase the oral bioavailability of tangeretin. Mol. Pharm. 2015, submitted for publication.
26. Blanquet, S.; Zeijdner, E.; Beyssac, E.; Meunier, J.-P.; Denis, S.; Havenaar, R.; Alric, M. A dynamic artificial gastrointestinal system for studying the behavior of orally administered drug dosage forms under various physiological conditions Pharm. Res. 2004, 21 (4) 585-591
27. Zhao, Q.; Lan, Y.; Xia, C.; Rogers, M. A.; Huang, Q. Comparison of in vitro models in determining bioaccessibility of nutraceuticals: the case of coenzyme Q10. J. Funct. Foods 2015, submitted for publication.
28. Lin, J. H.; Chiba, M.; Baillie, T. A. Is the role of the small intestine in first-pass metabolism overemphasized? Pharm. Rev. 1999, 51 (2) 135-158
29. Pelkonen, O.; Boobis, A. R.; Gundert-Remy, U. In vitro prediction of gastrointestinal absorption and bioavailability: an experts meeting report Eur. J. Clin. Pharmacol. 2001, 57 (9) 621-629
30. Bouayed, J.; Hoffmann, L.; Bohn, T. Total phenolics, flavonoids, anthocyanins and antioxidant activity following simulated gastro-intestinal digestion and dialysis of apple varieties: bioaccessibility and potential uptake Food Chem. 2011, 128 (1) 14-21
31. Zhang, L.; Zheng, Y.; Chow, M. S. S.; Zuo, Z. Investigation of intestinal absorption and disposition of green tea catechins by Caco-2 monolayer model Int. J. Pharm. 2004, 287 (1-2) 1-12
32. Walle, U. K.; Galijatovic, A.; Walle, T. Transport of the flavonoid chrysin and its conjugated metabolites by the human intestinal cell line Caco-2 Biochem. Pharmacol. 1999, 58 (3) 431-438
33. Konishi, Y.; Kobayashi, S.; Shimizu, M. Transepithelial transport of p -coumaric acid and gallic acid in Caco-2 cell monolayers Biosci., Biotechnol., Biochem. 2003, 67 (11) 2317-2324
34. Chabane, M. N.; Al Ahmad, A.; Peluso, J.; Muller, C. D.; Ubeaud, G. Quercetin and naringenin transport across human intestinal Caco-2 cells J. Pharm. Pharmacol. 2009, 61 (11) 1473-1483
35. Boyer, J.; Brown, D.; Liu, R. H. In vitro digestion and lactase treatment influence uptake of quercetin and quercetin glucoside by the Caco-2 cell monolayer Nutr. J. 2005, 4, 1
36. Hubatsch, I.; Ragnarsson, E. G. E.; Artursson, P. Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers Nat. Protoc. 2007, 2 (9) 2111-2119
37. Levy, E.; Mehran, M.; Seidman, E. Caco-2 cells as a model for intestinal lipoprotein synthesis and secretion FASEB J. 1995, 9 (8) 626-635
38. Seeballuck, F.; Lawless, E.; Ashford, M. B.; ODriscoll, C. M. Stimulation of triglyceride-rich lipoprotein secretion by polysorbate 80: in vitro and in vivo correlation using Caco-2 cells and a cannulated rat intestinal lymphatic model Pharm. Res. 2004, 21 (12) 2320-2326
39. Simmons, A. L.; Chitchumroonchokchai, C.; Vodovotz, Y.; Failla, M. L. Isoflavone retention during processing, bioaccessibility, and transport by Caco-2 cells: effects of source and amount of fat in a soy soft pretzel J. Agric. Food Chem. 2012, 60 (49) 12196-12203
40. Bailey, C. A.; Bryla, P.; Malick, A. W. The use of the intestinal epithelial cell culture model, Caco-2, in pharmaceutical development Adv. Drug Deliver. Rev. 1996, 22 (1-2) 85-103
41. Zakeri-Milani, P.; Valizadeh, H.; Tajerzadeh, H.; Azarmi, Y.; Islambolchilar, Z.; Barzegar, S.; Barzegar-Jalali, M. Predicting human intestinal permeability using single-pass intestinal perfusion in rat J. Pharm. Pharm. Sci. 2007, 10 (3) 368-379
42. Fagerholm, U.; Johansson, M.; Lennernas, H. Comparison between permeability coefficients in rat and human jejunum Pharm. Res. 1996, 13 (9) 1336-1342
43. Wilkinson, G. R. Drug metabolism and variability among patients in drug response New Engl. J. Med. 2005, 352 (21) 2211-2221
44. Ding, X. X.; Kaminsky, L. S. Human extrahepatic cytochromes P450: function in xenobiotic metabolism and tissue-selective chemical toxicity in the respiratory and gastrointestinal tracts Annu. Rev. Pharmacol. 2003, 43, 149-173
45. Botto, F.; Seree, E.; Elkhyari, S.; Desousa, G.; Massacrier, A.; Placidi, M.; Cau, P.; Pellet, W.; Rahmani, R.; Barra, Y. Tissue-specific expression and methylation of the human Cyp2e1 gene Biochem. Pharmacol. 1994, 48 (6) 1095-1103
46. Guengerich, F. P. Cytochrome p450 and chemical toxicology Chem. Res. Toxicol. 2007, 21 (1) 70-83
47. Siess, M. H.; Leclerc, J.; Canivenc-Lavier, M. C.; Rat, P.; Suschetet, M.; Thanou, J. C.; Verhoef; Junginger, H. E. Heterogenous effects of natural flavonoids on monooxygenase activities in human and rat liver microsomes Toxicol. Appl. Pharmacol. 1995, 130, 73-78
48. Nielsen, S. E.; Breinholt, V.; Justesen, U.; Cornett, C.; Dragsted, L. O. In vitro biotransformation of flavonoids by rat liver microsomes Xenobiotica 1998, 28 (4) 389-401
49. Canivenclavier, M. C.; Brunold, C.; Siess, M. H.; Suschetet, M. Evidence for tangeretin O-demethylation by rat and human liver-microsomes Xenobiotica 1993, 23 (3) 259-266
50. Bursztyka, J.; Perdu, E.; Tulliez, J.; Debrauwer, L.; Delous, G.; Canlet, C.; De, S. G.; Rahmani, R.; Benfenati, E.; Cravedi, J. P. Comparison of genistein metabolism in rats and humans using liver microsomes and hepatocytes Food Chem. Toxicol. 2008, 46 (3) 939-948
51. Boxenbaum, H. Interspecies scaling, allometry, physiological time, and the ground plan of pharmacokinetics J. Pharmacokinet. Biopharm. 1982, 10 (2) 201-225
52. Dedrick, R.; Bischoff, K. B.; Zaharko, D. S. Interspecies correlation of plasma concentration history of methotrexate (NSC-740) Cancer Chemother. Rep. 1970, 54 (2) 95-101
53. Obach, R. S.; Baxter, J. G.; Liston, T. E.; Silber, B. M.; Jones, B. C.; MacIntyre, F.; Rance, D. J.; Wastall, P. The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data J. Pharmacol. Exp. Ther. 1997, 283 (1) 46-58
54. Vallejo, F.; Larrosa, M.; Escudero, E.; Zafrilla, M. P.; Cerda, B.; Boza, J.; Garcia-Conesa, M. T.; Espin, J. C.; Tomas-Barberan, F. A. Concentration and solubility of flavanones in orange beverages affect their bioavailability in humans J. Agric. Food Chem. 2010, 58 (10) 6516-6524
55. Piskula, M. K.; Terao, J. Quercetins solubility affects its accumulation in rat plasma after oral administration J. Agric. Food Chem. 1998, 46 (10) 4313-4317
56. Das, S.; Lin, H. S.; Ho, P. C.; Ng, K. Y. The impact of aqueous solubility and dose on the pharmacokinetic profiles of resveratrol Pharm. Res. 2008, 25 (11) 2593-2600
57. Chen, X.; Yin, O. Q.; Zuo, Z.; Chow, M. S. Pharmacokinetics and modeling of quercetin and metabolites Pharm. Res. 2005, 22 (6) 892-901
58. Hou, Y.; Chao, P.; Ho, H.; Wen, C.; Hsiu, S. Profound difference in pharmacokinetics between morin and its isomer quercetin in rats J. Pharm. Pharmacol. 2003, 55 (2) 199-203
59. Reinboth, M.; Wolffram, S.; Abraham, G.; Ungemach, F. R.; Cermak, R. Oral bioavailability of quercetin from different quercetin glycosides in dogs Br. J. Nutr. 2010, 104 (2) 198-203
60. Cermak, R.; Landgraf, S.; Wolffram, S. The bioavailability of quercetin in pigs depends on the glycoside moiety and on dietary factors J. Nutr. 2003, 133 (9) 2802-2807
61. Gugler, R.; Leschik, M.; Dengler, H. Disposition of quercetin in man after single oral and intravenous doses Eur. J. Clin. Pharmacol. 1975, 9 (2-3) 229-234
62. Goldberg, D. M.; Yan, J.; Soleas, G. J. Absorption of three wine-related polyphenols in three different matrices by healthy subjects Clin. Biochem. 2003, 36 (1) 79-87
63. Moon, Y. J.; Wang, L.; DiCenzo, R.; Morris, M. E. Quercetin pharmacokinetics in humans Biopharm. Drug Dispos. 2008, 29 (4) 205-217
64. Li, J.; Jiang, Y. Y.; Wen, J.; Fan, G. R.; Wu, Y. T.; Zhang, C. A rapid and simple HPLC method for the determination of curcumin in rat plasma: assay development, validation and application to a pharmacokinetic study of curcumin liposome Biomed. Chromatogr. 2009, 23 (11) 1201-1207
65. Liu, A. C.; Lou, H. X.; Zhao, L. X.; Fan, P. H. 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. 2006, 40 (3) 720-727
66. Hu, L. D.; Jia, Y. H.; Niu, F.; Jia, Z.; Yang, X.; Jiao, K. L. Preparation and enhancement of oral bioavailability of curcumin using microemulsions vehicle J. Agric. Food Chem. 2012, 60 (29) 7137-7141
67. Liu, Z. F.; Chiu, M.; Wang, J.; Chen, W.; Yen, W.; Fan-Havard, P.; Yee, L. D.; Chan, K. K. Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice Cancer Chemother. Pharm. 2012, 69 (3) 679-689
68. Kakkar, V.; Singh, S.; Singla, D.; Kaur, I. P. Exploring solid lipid nanoparticles to enhance the oral bioavailability of curcumin Mol. Nutr. Food Res. 2011, 55 (3) 495-503
69. Wan, S. X.; Sun, Y. Q.; Qi, X. X.; Tan, F. P. Improved bioavailability of poorly water-soluble drug curcumin in cellulose acetate solid dispersion AAPS PharmSciTech 2012, 13 (1) 159-166
70. Pietta, P.; Simonetti, P.; Gardana, C.; Brusamolino, A.; Morazzoni, P.; Bombardelli, E. Relationship between rate and extent of catechin absorption and plasma antioxidant status Biochem. Mol. Biol. Int. 1998, 46 (5) 895-903
71. Dube, A.; Nicolazzo, J. A.; Larson, I. Chitosan nanoparticles enhance the plasma exposure of (-)-epigallocatechin gallate in mice through an enhancement in intestinal stability Eur. J. Pharm. Sci. 2011, 44 (3) 422-426