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Current Nutraceuticals

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ISSN (Print): 2665-9786
ISSN (Online): 2665-9794

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Research Article

Oral Controlled Delivery of Natural Compounds Using Food-Grade Polymer Microparticles

Author(s): Claudia Curcio, Angela Bonaccorso, Teresa Musumeci and Rosario Pignatello*

Volume 2, Issue 2, 2021

Published on: 26 November, 2020

Page: [145 - 153] Pages: 9

DOI: 10.2174/2665978601999201126212614

Abstract

Background: Targeted drug delivery to the colon is a strategic approach for the local cure of inflammatory bowel diseases (IBD) and other syndromes like colon cancer. Research is actively focusing on possible alternative and safer therapies to conventional drugs, based on herbal remedies and other natural products. In particular, colon-targeted drug delivery systems (CDDS) offer the opportunity to protect the active compound along the way to the colon. Drug release and absorption, and even degradation, should not occur in the stomach and small bowel, but a selective release should start once the drug moves to the colonic area.

Objective: This work aims at evaluating the gastro-resistant properties of new food-grade methacrylic resins (Eudraguard®), used not as coating materials, but used after the formation of microparticles to achieve a delayed and targeted release of a model drug, resveratrol (RVT), to the ileo-colonic area.

Methods: Microparticles were produced by an emulsion-solvent evaporation technique (ESE) and characterized by solid-state analytical methods. RVT release profiles were assessed in vitro using a pH-change procedure, able to simulate the transit of the carrier along the gastro-intestinal tract.

Results: Eudraguard® Biotic can form microparticles with a very high encapsulation efficiency for RVT; the polymeric matrix was able to limit the diffusion of the drug at gastric and gut pH conditions, while a higher release was achieved at pH 7.4. Conversely, using the Eudraguard® Control resin, alone or blended with the former polymer, did not allow to achieve a controlled release of RVT at the various pH values.

Conclusion: Food-grade Eudraguard® matrices deserve further investigations as polymeric materials for the preparation of micrometric matrices or pellets for the oral controlled release of natural active ingredients to the ileo-colonic area.

Keywords: Colonic delivery, resveratrol, food supplements, Eeudraguard copolymers, pH-controlled delivery, RVT.

Graphical Abstract

[1]
Yao M, McClements DJ, Xiao H. Improving oral bioavailability of nutraceuticals by engineered nanoparticle-based delivery systems. Curr Opin Food Sci 2015; 2: 14-9.
[http://dx.doi.org/10.1016/j.cofs.2014.12.005]
[2]
Ashwini C, Vaishali K, Ram S, Ganesh B, Digambar N. Role of nutraceuticals in various diseases: A comprehensive review. Int J Res Pharm Chem 2013; 3(2): 290-9.
[3]
Nasri H, Baradaran A, Shirzad H, Rafieian-Kopaei M. New concepts in nutraceuticals as alternative for pharmaceuticals. Int J Prev Med 2014; 5(12): 1487-99.
[PMID: 25709784]
[4]
Ting Y, Jiang Y, Ho CT, Huang Q. Common delivery systems for enhancing in vivo bioavailability and biological efficacy of nutraceuticals. J Funct Foods 2014; 7: 112-28.
[http://dx.doi.org/10.1016/j.jff.2013.12.010]
[5]
Knowles SR, Graff LA, Wilding H, Hewitt C, Keefer L, Mikocka-Walus A. Quality of life in Inflammatory Bowel Disease: a systematic review and meta-analyses - Part I. Inflamm Bowel Dis 2018; 24(4): 742-51.
[http://dx.doi.org/10.1093/ibd/izx100] [PMID: 29562277]
[6]
Uranga JA, López-Miranda V, Lombó F, Abalo R. Food, nutrients and nutraceuticals affecting the course of inflammatory bowel disease. Pharmacol Rep 2016; 68(4): 816-26.
[http://dx.doi.org/10.1016/j.pharep.2016.05.002] [PMID: 27267792]
[7]
Burger D, Travis S. Conventional medical management of inflammatory bowel disease. Gastroenterology 2011; 140(6): 1827-1837.e2.
[http://dx.doi.org/10.1053/j.gastro.2011.02.045] [PMID: 21530749]
[8]
Chan HC, Ng SC. Emerging biologics in inflammatory bowel disease. J Gastroenterol 2017; 52(2): 141-50.
[http://dx.doi.org/10.1007/s00535-016-1283-0] [PMID: 27832357]
[9]
Sinhmar GK, Shah NN, Chokshi NV, Khatri HN, Patel MM. Process, optimization, and characterization of budesonide-loaded nanostructured lipid carriers for the treatment of inflammatory bowel disease. Drug Dev Ind Pharm 2018; 44(7): 1078-89.
[http://dx.doi.org/10.1080/03639045.2018.1434194] [PMID: 29376433]
[10]
Chourasia MK, Jain SK. Pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Pharm Sci 2003; 6(1): 33-66.
[PMID: 12753729]
[11]
Prasanth VV, Jayaprakash R, Sam TM. Colon specific Drug Delivery Systems: a review on various pharmaceutical approaches. J Appl Pharm Sci 2012; 2(1): 163-9.
[12]
Lautenschläger C, Schmidt C, Fischer D, Stallmach A. Drug delivery strategies in the therapy of inflammatory bowel disease. Adv Drug Deliv Rev 2014; 71: 58-76.
[http://dx.doi.org/10.1016/j.addr.2013.10.001] [PMID: 24157534]
[13]
Eisele J, Haynes G, Kreuzer K, Hall C. Toxicological assessment of Anionic Methacrylate Copolymer: I. Characterization, bioavailability and genotoxicity. Regul Toxicol Pharmacol 2016; 82: 39-47.
[http://dx.doi.org/10.1016/j.yrtph.2016.11.009] [PMID: 27825834]
[14]
EFSA Panel on Food Additives and Nutrient Sources added to Food (ANS). Scientific Opinion on the safety of anionic methacrylate copolymer for the proposed uses as a food additive. EFSA J 2010; 8: 1656.
[http://dx.doi.org/10.2903/j.efsa.2010.1656]
[15]
Pignatello R, Consoli P, Puglisi G. In vitro release kinetics of Tolmetin from tabletted Eudragit microparticles. J Microencapsul 2000; 17(3): 373-83.
[http://dx.doi.org/10.1080/026520400288337] [PMID: 10819424]
[16]
Pignatello R, Amico D, Chiechio S, Spadaro C, Puglisi G, Giunchedi P. Preparation and analgesic activity of Eudragit RS100 microparticles containing diflunisal. Drug Deliv 2001; 8(1): 35-45.
[http://dx.doi.org/10.1080/107175401300002748] [PMID: 11280442]
[17]
Pignatello R, Bucolo C, Spedalieri G, Maltese A, Puglisi G. Flurbiprofen-loaded acrylate polymer nanosuspensions for ophthalmic application. Biomaterials 2002; 23(15): 3247-55.
[http://dx.doi.org/10.1016/S0142-9612(02)00080-7] [PMID: 12102196]
[18]
Pecora TMG, Cianciolo S, Catalfo A, et al. Preparation, characterization and photostability assessment of curcumin microencapsulated within methacrylic copolymers. J Drug Deliv Sci Technol 2016; 33: 88-97.
[http://dx.doi.org/10.1016/j.jddst.2016.03.013]
[19]
Paolino D, Vero A, Cosco D, et al. Improvement of oral bioavailability of curcumin upon microencapsulation with methacrylic copolymers. Front Pharmacol 2016; 7: 485.
[http://dx.doi.org/10.3389/fphar.2016.00485] [PMID: 28066239]
[20]
Yus C, Gracia R, Larrea A, et al. Targeted release of probiotics from enteric microparticulated formulations. Polymers (Basel) 2019; 11(10): 1668.
[http://dx.doi.org/10.3390/polym11101668] [PMID: 31614915]
[21]
Baur JA, Sinclair DA. Therapeutic potential of resveratrol: the in vivo evidence. Nat Rev Drug Discov 2006; 5(6): 493-506.
[http://dx.doi.org/10.1038/nrd2060] [PMID: 16732220]
[22]
Nunes S, Danesi F, Del Rio D, Silva P. Resveratrol and inflammatory bowel disease: the evidence so far. Nutr Res Rev 2018; 31(1): 85-97.
[http://dx.doi.org/10.1017/S095442241700021X] [PMID: 29191255]
[23]
Walle T, Hsieh F, DeLegge MH, Oatis JE Jr, Walle UK. High absorption but very low bioavailability of oral resveratrol in humans. Drug Metab Dispos 2004; 32(12): 1377-82.
[http://dx.doi.org/10.1124/dmd.104.000885] [PMID: 15333514]
[24]
Devi P, Sharma P, Rathore C, Negi P. Novel drug delivery systems of resveratrol to bioavailability and therapeutic effects. Resveratrol - Adding Life to Years, Not Adding Years to Life. London, UK: IntechOpen 2019; pp. 25-45.
[http://dx.doi.org/10.5772/intechopen.79739]
[25]
Chimento A, De Amicis F, Sirianni R, et al. Progress to improve oral bioavailability and beneficial effects of resveratrol. Int J Mol Sci 2019; 20(6): 1381.
[http://dx.doi.org/10.3390/ijms20061381] [PMID: 30893846]
[26]
Andishmand H, Tabibiazar M, Mohammadifar MA, Hamishehkar H. Pectin-zinc-chitosan-polyethylene glycol colloidal nano-suspension as a food grade carrier for colon targeted delivery of resveratrol. Int J Biol Macromol 2017; 97: 16-22.
[http://dx.doi.org/10.1016/j.ijbiomac.2016.12.087] [PMID: 28064058]
[27]
Curcio C, Greco AS, Rizzo S, et al. Development, optimization and characterization of Eudraguard®-based microparticles for colon delivery. Pharmaceuticals (Basel) 2020; 13(6): 131.
[http://dx.doi.org/10.3390/ph13060131] [PMID: 32599861]
[28]
Agarwal A, Kharb V, Saharan VA. Process optimisation, characterisation and evaluation of resveratrol-phospholipid complexes using Box-Behnken statistical design. Int Curr Pharm J 2014; 3(7): 301-8.
[http://dx.doi.org/10.3329/icpj.v3i7.19079]

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