Design of a pectin-based microparticle formulation using zinc ions as the cross-linking agent and glutaraldehyde as the hardening agent for colonic-specific delivery of resveratrol: In vitro and in vivo evaluations

Journal of Drug Targeting

Volumn 19, Issue 6, 2011, Pages 446-457

  Das, Surajit ^a   Ng, Ka Yun ^a   Ho, Paul C ^a  

^a NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

Author keywords

colon specific; glutaraldehyde; microparticles; Resveratrol; zinc pectinate

Indexed keywords

GLUTARALDEHYDE; PECTIN; RESVERATROL; UNCLASSIFIED DRUG; ZINC ION; ZINC PECTINATE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COLON; CONTROLLED STUDY; CROSS LINKING; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG RELEASE; DRUG STABILITY; DRUG STRUCTURE; ENCAPSULATION; INFRARED SPECTROSCOPY; MALE; MAXIMUM PLASMA CONCENTRATION; MOISTURE; NONHUMAN; PARTICLE SIZE; PH; PRIORITY JOURNAL; PRODUCTIVITY; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; COLON; CROSS-LINKING REAGENTS; DRUG CARRIERS; DRUG DESIGN; DRUG STABILITY; GLUTARAL; MALE; MICROSCOPY, ELECTRON, SCANNING; PARTICLE SIZE; PECTINS; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; STILBENES; SURFACE PROPERTIES; TISSUE DISTRIBUTION;

EID: 79958773927     PISSN: 1061186X     EISSN: 10292330     Source Type: Journal    
DOI: 10.3109/1061186X.2010.504272     Document Type: Article

References (32)

1. Atyabi F, Majzoob S, Iman M, Salehi M, Dorkoosh F. (2005). In vitro evaluation and modification of pectinate gel beads containing trimethyl chitosan, as a multi-particulate system for delivery of water-soluble macromolecules to colon. Carbohydr Polym, 61, 39-51. (Pubitemid 40774011)
2. Basit AW. (2005). Advances in colonic drug delivery. Drugs, 65, 1991-2007. (Pubitemid 41324059)
3. Baur JA, Pearson KJ, Price NL, Jamieson HA, Lerin C, Kalra A, Prabhu VV, Allard JS, Lopez-Lluch G, Lewis K, Pistell PJ, Poosala S, Becker KG, Boss O, Gwinn D, Wang M, Ramaswamy S, Fishbein KW, Spencer RG, Lakatta EG, Le Couteur D, Shaw RJ, Navas P, Puigserver P, Ingram DK, de Cabo R, Sinclair DA. (2006). Resveratrol improves health and survival of mice on a high-calorie diet. Nature, 444, 337-342. (Pubitemid 44764104)
4. Baur JA, Sinclair DA. (2006). Therapeutic potential of resveratrol: the in vivo evidence. Nat Rev Drug Discov, 5, 493-506. (Pubitemid 44136961)
5. Cardoso SM, Coimbra MA, Lopes da Silva JA. (2003). Temperature dependence of the formation and melting of pectin-Ca 2+ networks: A rheological study. Food Hydrocolloids, 17, 801-807.
6. Chambin O, Dupuis G, Champion D, Voilley A, Pourcelot Y. (2006). Colon-specific drug delivery: Influence of solution reticulation properties upon pectin beads performance. Int J Pharm, 321, 86-93. (Pubitemid 44262458)
7. Chang C, Wang ZC, Quan CY, Cheng H, Cheng SX, Zhang XZ, Zhuo RX. (2007). Fabrication of a novel pH-sensitive glutaraldehyde crosslinked pectin nanogel for drug delivery. J Biomater Sci Polym Ed, 18, 1591-1599. (Pubitemid 350014876)
8. Das S, Lin HS, Ho PC, Ng KY. (2008). The impact of aqueous solubility and dose on the pharmacokinetic profiles of resveratrol. Pharm Res, 25, 2593-2600.
9. Das S, Ng KY. (2010). Colon-specific delivery of resveratrol: optimization of multi-particulate calcium-pectinate carrier. Int J Pharm, 385, 20-28.
10. Das S, Ng KY. (2010). Resveratrol-loaded calcium-pectinate beads: effects of formulation parameters on drug release and bead characteristics. J Pharm Sci, 99, 840-860.
11. Das S, Ng KY, Ho PC. (2010). Formulation and optimization of zincpectinate beads for the controlled delivery of resveratrol. AAPS PharmSciTech, 11, 729-742.
12. Dupuis G, Chambin O, Génelot C, Champion D, Pourcelot Y. (2006). Colonic drug delivery: influence of cross-linking agent on pectin beads properties and role of the shell capsule type. Drug Dev Ind Pharm, 32, 847-855. (Pubitemid 44266769)
13. El-Gibaly I. (2002). Oral delayed-release system based on Zn-pectinate gel (ZPG) microparticles as an alternative carrier to calcium pectinate beads for colonic drug delivery. Int J Pharm, 232, 199-211. (Pubitemid 34076766)
14. Friend DR. (2005). New oral delivery systems for treatment of inflammatory bowel disease. Adv Drug Deliv Rev, 57, 247-265. (Pubitemid 39536101)
15. Gescher AJ, Steward WP. (2003). Relationship between mechanisms, bioavailibility, and preclinical chemopreventive efficacy of resveratrol: a conundrum. Cancer Epidemiol Biomarkers Prev, 12, 953-957. (Pubitemid 37310248)
16. Gilsenan PM, Richardson RK, Morris ER. (2000). Thermally reversible acid-induced gelation of low-methoxy pectin. Carbohydr Polym 41:339-349. (Pubitemid 30529944)
17. Grant GT, Morris ER, Rees DA. (1973). Biological interactions between polysaccharides and divalent cations: The egg box model. FEBS Letters, 32, 195-198.
18. Kaldas MI, Walle UK, Walle T. (2003). Resveratrol transport and metabolism by human intestinal Caco-2 cells. J Pharm Pharmacol, 55, 307-312. (Pubitemid 36410351)
19. Liu L, Fishman ML, Kost J, Hicks KB. (2003). Pectin-based systems for colon-specific drug delivery via oral route. Biomaterials, 24, 3333-3343. (Pubitemid 36581891)
20. Lootens D, Capel F, Durand D, Nicolai T, Boulenguer P, Langendorff V. (2003). Influence of pH, Ca concentration, temperature and amidation on the gelation of low methoxyl pectin. Food Hydrocolloids, 17, 237-244.
21. Maestrelli F, Cirri M, Corti G, Mennini N, Mura P. (2008). Development of enteric-coated calcium pectinate microspheres intended for colonic drug delivery. Eur J Pharm Biopharm, 69, 508-518.
22. Maestrelli F, Zerrouk N, Cirri M, Mennini N, Mura P. (2008). Microspheres for colonic delivery of ketoprofen-hydroxypropylbeta-cyclodextrin complex. Eur J Pharm Sci, 34, 1-11.
23. Maier-Salamon A, Hagenauer B, Wirth M, Gabor F, Szekeres T, Jäger W. (2006). Increased transport of resveratrol across monolayers of the human intestinal Caco-2 cells is mediated by inhibition and saturation of metabolites. Pharm Res, 23, 2107-2115.
24. Marier JF, Vachon P, Gritsas A, Zhang J, Moreau JP, Ducharme MP. (2002). Metabolism and disposition of resveratrol in rats: extent of absorption, glucuronidation, and enterohepatic recirculation evidenced by a linked-rat model. J Pharmacol Exp Ther, 302, 369-373. (Pubitemid 34680460)
25. Martín AR, Villegas I, La Casa C, de la Lastra CA. (2004). Resveratrol, a polyphenol found in grapes, suppresses oxidative damage and stimulates apoptosis during early colonic inflammation in rats. Biochem Pharmacol, 67, 1399-1410. (Pubitemid 38315105)
26. Martín AR, Villegas I, Sánchez-Hidalgo M, de la Lastra CA. (2006). The effects of resveratrol, a phytoalexin derived from red wines, on chronic inflammation induced in an experimentally induced colitis model. Br J Pharmacol, 147, 873-885.
27. Murata Y, Miyashita M, Kofuji K, Miyamoto E, Kawashima S. (2004). Drug release properties of a gel bead prepared with pectin and hydrolysate. J Control Release, 95, 61-66. (Pubitemid 38167679)
28. Schneider Y, Duranton B, Gossé F, Schleiffer R, Seiler N, Raul F. (2001). Resveratrol inhibits intestinal tumorigenesis and modulates hostdefense-related gene expression in an animal model of human familial adenomatous polyposis. Nutr Cancer, 39, 102-107. (Pubitemid 32880955)
29. Sriamornsak P. (1999). Effect of calcium concentration, hardening agent and drying condition on release characteristics of oral proteins from calcium pectinate gel beads. Eur J Pharm Sci, 8, 221-227. (Pubitemid 29324650)
30. Sriamornsak P, Nunthanid J. (1999). Calcium pectinate gel beads for controlled release drug delivery: II. Effect of formulation and processing variables on drug release. J Microencapsul, 16, 303-313. (Pubitemid 29191814)
31. Tessitore L, Davit A, Sarotto I, Caderni G. (2000). Resveratrol depresses the growth of colorectal aberrant crypt foci by affecting bax and p21(CIP) expression. Carcinogenesis, 21, 1619-1622. (Pubitemid 30608219)
32. Walle T, Hsieh F, DeLegge MH, Oatis JE Jr, Walle UK. (2004). High absorption but very low bioavailability of oral resveratrol in humans. Drug Metab Dispos, 32, 1377-1382. (Pubitemid 39564557)