Electrosprayed Chitosan Coated Alginate-Pectin Beads as Potential System for Colon- Targeted Delivery of Ellagic Acid.

BACKGROUND Ellagic acid (EA), a potent dietary antioxidant, has limited bioavailability due to its rapid absorption in the stomach and small intestine, and EA is transformed to more bioavailable compounds, urolithins, in the colon. An encapsulation system that sustain the release of EA in the gastrointestinal system and deliver more EA into the colon could improve the oral bioavailability of EA. Electrosprayed EA-loaded alginate-pectin beads were produced and coated with low (LC) and high molecular weight chitosan (HC). The EA release from uncoated and coated beads under simulated gastrointestinal conditions was evaluated. The samples were characterized by particle size, gel strength, SEM, and FT-IR analysis. RESULTS The encapsulation efficiency (EE%) of EA was ranged from 49.53 to 69.85% for uncoated beads, elevated up to 86.50% by coating, and LC coating provided higher EE%. The pectin addition into alginate and chitosan coating reduced the gel strength, changed the size depending on the molecular weight of chitosan. SEM images of pectin added beads showed fewer cracks but more wrinkles, and chitosan coating presented more aggregated surfaces. The ionic interaction of alginate-pectin-chitosan and the entrapment of EA were confirmed by FT-IR. In the gastric medium, EA release was very low from uncoated beads (15.2-19.8%), and totally restricted by chitosan coating. In the intestinal stage, EA release from LC-coated alginate-pectin beads was only 18%, and it was between 55-65% for uncoated or HC-coated counterparts. CONCLUSION The LC-coated alginate-pectin beads could be further explored as a potential system for colon-targeted delivery of EA. This article is protected by copyright. All rights reserved.

[1]  J. Espín,et al.  Ellagitannins and Their Gut Microbiota‐Derived Metabolites: Urolithins , 2020 .

[2]  Bingcan Chen,et al.  Alginate-based double-network hydrogel improves the viability of encapsulated probiotics during simulated sequential gastrointestinal digestion: Effect of biopolymer type and concentrations. , 2020, International journal of biological macromolecules.

[3]  I. Faraoni,et al.  Strategies to improve ellagic acid bioavailability: from natural or semisynthetic derivatives to nanotechnological approaches based on innovative carriers , 2020, Nanotechnology.

[4]  S. Jafari,et al.  Morphology and microstructural analysis of bioactive-loaded micro/nanocarriers via microscopy techniques; CLSM/SEM/TEM/AFM. , 2020, Advances in colloid and interface science.

[5]  F. Turrini,et al.  Formulation Strategies to Improve Oral Bioavailability of Ellagic Acid , 2020, Applied Sciences.

[6]  M. Sarker,et al.  Taste masking of paracetamol encapsulated in chitosan-coated alginate beads , 2020, Journal of Drug Delivery Science and Technology.

[7]  Asma Sadat Vaziri,et al.  Potential effects of alginate–pectin biocomposite on the release of folic acid and their physicochemical characteristics , 2020, Journal of Food Science and Technology.

[8]  Sreeprasad T. Sreenivasan,et al.  Chitosan-Ellagic acid Nanohybrid for mitigating rotenone-induced oxidative stress. , 2020, ACS applied materials & interfaces.

[9]  Jie Zhu,et al.  Comparative study on the self-assembly of pectin and alginate molecules regulated by calcium ions investigated by atomic force microscopy. , 2020, Carbohydrate polymers.

[10]  E. Vatankhah,et al.  Experimental investigation into size and sphericity of alginate micro-beads produced by electrospraying technique: Operational condition optimization. , 2019, Carbohydrate polymers.

[11]  M. Hubinger,et al.  Anthocyanins from jussara (Euterpe edulis Martius) extract carried by calcium alginate beads pre-prepared using ionic gelation , 2019, Powder Technology.

[12]  Botao Song.  Lotus leaf-inspired design of calcium alginate particles with superhigh drug encapsulation efficiency and pH responsive release. , 2018, Colloids and surfaces. B, Biointerfaces.

[13]  N. Tucker,et al.  Electrospray-assisted encapsulation of caffeine in alginate microhydrogels. , 2018, International journal of biological macromolecules.

[14]  D. Mcclements,et al.  Controlled-release of antacids from biopolymer microgels under simulated gastric conditions: Impact of bead dimensions, pore size, and alginate/pectin ratio. , 2018, Food research international.

[15]  C. Freire,et al.  Bioactive chitosan/ellagic acid films with UV-light protection for active food packaging , 2017 .

[16]  J. Teixeira,et al.  Effect of alginate molecular weight and M/G ratio in beads properties foreseeing the protection of probiotics , 2017 .

[17]  Mohamed A. Shaker,et al.  Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles , 2017, International journal of nanomedicine.

[18]  H. McCarthy,et al.  Influence of alginate backbone on efficacy of thermo-responsive alginate-g-P(NIPAAm) hydrogel as a vehicle for sustained and controlled gene delivery. , 2017, Materials science & engineering. C, Materials for biological applications.

[19]  Soonkyu Chung,et al.  Improvements in Metabolic Health with Consumption of Ellagic Acid and Subsequent Conversion into Urolithins: Evidence and Mechanisms. , 2016, Advances in nutrition.

[20]  T. Klein,et al.  Evaluation of the impact of freezing preparation techniques on the characterisation of alginate hydrogels by cryo-SEM , 2016 .

[21]  G. Messaoud,et al.  Encapsulation of Lactococcus lactis subsp. lactis on alginate/pectin composite microbeads: Effect of matrix composition on bacterial survival and nisin release , 2016 .

[22]  E. Chan,et al.  Advances in fabricating spherical alginate hydrogels with controlled particle designs by ionotropic gelation as encapsulation systems , 2016 .

[23]  Praveen Kumar,et al.  Development and In Vitro Characterization of Capecitabine-Loaded Alginate–Pectinate–Chitosan Beads for Colon Targeting , 2016 .

[24]  H. Moghadam,et al.  Electrospray preparation of propranolol‐loaded alginate beads: Effect of matrix reinforcement on loading and release profile , 2015 .

[25]  S. Karlović,et al.  Improving the controlled delivery formulations of caffeine in alginate hydrogel beads combined with pectin, carrageenan, chitosan and psyllium. , 2015, Food chemistry.

[26]  Boonsri Kusuktham,et al.  Morphology and Property of Calcium Silicate Encapsulated with Alginate Beads , 2014, Silicon.

[27]  M. Corredig,et al.  A standardised static in vitro digestion method suitable for food - an international consensus. , 2014, Food & function.

[28]  D. Song,et al.  Microencapsulation of peppermint oil in an alginate–pectin matrix using a coaxial electrospray system , 2014 .

[29]  J. Weiss,et al.  Presence of electrostatically adsorbed polysaccharides improves spray drying of liposomes. , 2013, Journal of food science.

[30]  M. E. D. Silva,et al.  Natamycin release from alginate/pectin films for food packaging applications , 2012 .

[31]  Xiaoli Zhu,et al.  Encapsulation of probiotic Bifidobacterium longum BIOMA 5920 with alginate-human-like collagen and evaluation of survival in simulated gastrointestinal conditions. , 2011, International journal of biological macromolecules.

[32]  E. Chan,et al.  Comparison of alginate and pectin based beads for production of poultry probiotic cells. , 2011, Journal of bioscience and bioengineering.

[33]  Marisa Masumi Beppu,et al.  Natural-based plasticizers and biopolymer films: A review , 2011 .

[34]  P. Panichayupakaranant,et al.  Preparation method and stability of ellagic acid-rich pomegranate fruit peel extract , 2010, Pharmaceutical biology.

[35]  J. Espín,et al.  Interaction between phenolics and gut microbiota: role in human health. , 2009, Journal of agricultural and food chemistry.

[36]  P. Gowland,et al.  Investigation of alginate beads for gastro-intestinal functionality, Part 1: In vitro characterisation , 2009 .

[37]  J. Mano,et al.  Chitosan coated alginate beads containing poly(N-isopropylacrylamide) for dual-stimuli-responsive drug release. , 2008, Journal of biomedical materials research. Part B, Applied biomaterials.

[38]  David Heber,et al.  Pomegranate juice ellagitannin metabolites are present in human plasma and some persist in urine for up to 48 hours. , 2006, The Journal of nutrition.

[39]  M. R. Kumar,et al.  Analytical methods for assay of ellagic acid and its solubility studies. , 2006, Journal of pharmaceutical and biomedical analysis.

[40]  M. Phillips,et al.  Alginate–pectin microcapsules as a potential for folic acid delivery in foods , 2005, Journal of microencapsulation.

[41]  A. K. Anal,et al.  Chitosan-alginate multilayer beads for controlled release of ampicillin. , 2005, International journal of pharmaceutics.

[42]  Anne-Marie Hermansson,et al.  Microstructure and rheological behaviour of alginate/pectin mixed gels , 2003 .

[43]  M. Clifford.  Anthocyanins – nature, occurrence and dietary burden , 2000 .

[44]  G. Skjåk-Bræk,et al.  Microcapsules of alginate-chitosan. II. A study of capsule stability and permeability. , 1999, Biomaterials.

[45]  Chong-K. Kim,et al.  Biphasic release characteristics of dual drug-loaded alginate beads , 1998, Archives of pharmacal research.

[46]  G. Skjåk-Bræk,et al.  Microcapsules of alginate-chitosan--I. A quantitative study of the interaction between alginate and chitosan. , 1998, Biomaterials.

[47]  D. Poncelet,et al.  The influence of solution viscosities and surface tension on calcium-alginate microbead formation using dripping technique , 2017 .

[48]  J. Álvarez-Ramírez,et al.  Textural properties of alginate–pectin beads and survivability of entrapped Lb. casei in simulated gastrointestinal conditions and in yoghurt , 2010 .

[49]  Brian Ralph,et al.  Determination of the cation content of alginate thin films by FTi.r. spectroscopy , 1997 .

[50]  O. Smidsrod,et al.  Synergistic gelation of alginates and pectins , 1986 .