Chitosan-coated pectin beads: Characterization and in vitro release of mangiferin
Introduction
Dietary compounds with health benefits offer an excellent opportunity to improve public health. The list of these compounds, known as nutraceutical, is endless and includes vitamins, probiotics, bioactive peptides, antioxidants (Wildman, 2001).
Mangiferin, a xanthone glucoside (Fig. 1), is an active phytochemical present in various plants including Mangifera indica L. (Barreto et al., 2008). This phytochemical is recommended in the Indian system of medicine for the treatment of immuno-deficiency diseases such as arthritis, diabetes, hepatitis, cardiac and mental disorders (Sanchez et al., 2000). In Cuba, there is a mangiferin-enriched extract named Vimang, produced in industrial scale, mainly used as a nutritional supplement (Pardo-Andreu et al., 2006).
This xanthone glucoside has been reported to have analgesic and antioxidant activities (Dar et al., 2005), anti-allergic properties (Rivera et al., 2006), anthelminthic property (Garcia, Escalante, Delgado, Ubeira, & Leiro, 2003), gastro-protective effect (Carvalho et al., 2007), antitumor activity (Guha, Ghosal, & Chattopadhyay, 1996), and antiviral property (Yoosook, Bunyapraphatsara, Boonyakiat, & Kantasuk, 2000). Mangiferin was also used as foodstuffs for treating diabetes (Wada, 2007) and treating and preventing neurodegenerative diseases and aging symptoms (Matute et al., 2007). The bioactive can be considered as non-toxic as its reported oral LD50 value in mice was 400 mg/kg (Jagetia & Baiga, 2005).
The solubility in water of mangiferin is very low: 0.111 mg/mL (Wang, Deng, Li, & Wang, 2007). Some efforts were done in order to increase its solubility and bioavailability, such as embodying within cyclodextrin derivatives (Teng, Yu, Zhai, Li, & Liu, 2007), preparing an inclusion compound (Wang et al., 2007) or monosodium salt (Deng & Yuan, 2007). One strategy to preserve the chemical integrity and increase bioavailability for poorly water soluble food substrates is encapsulation (Duchateau & Klaffke, 2008). Encapsulation matrices provide maximal physical stability, protect ingredients against chemical degradation, and allow for precise control over the release of encapsulated components during mastication and digestion to maximize adsorption (Weiss et al., 2008).
Pectin is known in the food industry primarily as a gelling agent and is widely used in the production of jams and jellies, fruit juice, confectionery products, bakery fillings and for the stabilization of acidified milk drinks and yogurts (Willats, Knox, & Mikkelsen, 2006). Chemically, pectin is a family of complex heterogeneous oligosaccharides and polysaccharides. The dominant structural feature is a linear chain of poly-α-d-galacturonic acid with 1 → 4 linkages. In pectin from all sources, the carboxyl groups are partially in the methyl ester form. The degree of esterification (DE) varies depending on the source. This polysaccharide is non-toxic, not digested by gastric or intestinal enzymes and almost totally degraded by pectinolytic enzymes produced by the colonic microflora (Bourgeois, Gernet, Pradeau, Andremont, & Fattal, 2006).
Chitosan (copolymer of β-(1 → 4)-d-glucosamine and β-(1 → 4)-N-acetyl-d-glucosamine), is obtained from chitin – found in abundance in nature, mainly in carapace of crustaceans. The cationic polyelectrolyte nature of chitosan can also provide a strong electrostatic interaction with the mucus or a negatively charged mucosal surface. This mucoadhesive property may extend the time of residence of the sphere containing the bioactive in the gastric intestine (Kim, Park, Kim, & Cho, 2003).
Pectin capsules were used as a food carrier for the delivery of folic acid (Madziva, Kailasapathy, & Phillips, 2006). Pectin-based systems have been applied for colon-specific drug delivery via oral route (Liu, Fishman, Kost, & Hicks, 2003). The interaction between pectin and chitosan is known (Bernabé et al., 2005, Kamburova et al., 2008, Rashidova et al., 2004). These systems would be useful for colon-specific delivery of bioactive (Zhang & Lin, 2000), albumin delivery (Kim et al., 2003) and bimodal drug release (Macleod, Collett, & Fell, 1999).
In the present paper, pectin spheres coated with chitosan were prepared and characterized. The reacetylation of the chitosan coating wall was done as a way to protect beads from dissolving in gastric medium. These beads were tested on the controlled release of mangiferin.
Section snippets
Materials
Citric pectin (P) samples were obtained from Vetec – Chemicals. Chitosan (C) with molar mass 7.82 × 104 g/mol and degree of deacetylation of 81 ± 1% was obtained from Quitoquímica – Chemicals and characterized by Magalhães et al. (2009). Mangiferin (M) sample was obtained and characterized by Barreto et al. (2008). All other chemicals used were of analytical grade.
Preparation of beads of pectin/calcium and pectin/calcium/chitosan
The procedure for the preparation of particles of pectin/calcium and pectin/calcium/chitosan is similar to that used by Sriamornsak
GPC
A single and wide peak with no shoulders is present in the chromatogram of pectin sample (data not showed). The peak molar mass (Mpk) of polysaccharide was estimated using pullulan (a neutral polysaccharide) standard plot. Taking into account that the pectin is a polyelectrolyte, it is expected that it elutes at a lower volume than a neutral macromolecule with the same molar mass. This is due to chain stiffening and extent, as a consequence of electrostatic repulsion of carboxylate groups. The
Conclusion
Microspheres of pectin/Ca/chitosan were prepared. The layer of chitosan is in the range of 5–15 μm thick in a bead of approximately 660 μm of diameter. Chitosan was reacetylated and the new bead was successfully used to load mangiferin. The reacetylation causes deformation on the bead shape, which becomes more irregular and rough. The yields on the preparation of beads varied between 19 and 36%, being the bead with the lowest degree of reacetylation and with mangiferin incorporated in pectin
Acknowledgements
The authors would like to express their thanks to financial support by CNPq, CAPES, FUNCAP, and also to Rede Nanoglicobiotec/MCT/CNPq.
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