Abstract: Pectinate gel beads containing Thai mango seed kernel extract (MSKE, cultivar ‘Fahlun’) were developed and characterised for the purpose of colon-targeted delivery. The MSKE-loaded pectinate beads were prepared using ionotropic gelation with varying pectin-to-MSKE ratios, MSKE concentrations, and concentrations of two cross-linkers (calcium chloride and zinc acetate). The formulated beads were spherical in shape and ranged in size between 1.13 mm and 1.88 mm. Zinc-pectinate (ZPG) beads containing high amounts of MSKE showed complete entrapment efficiency (EE) of MSKE (100%), while calcium-pectinate (CPG) beads demonstrated 70% EE. The in vitro release tests indicated that MSKE-loaded CPG beads were unstable in both simulated gastric medium (SGM) and simulated intestinal medium (SIM), while MSKE-loaded ZPG beads were stable in SIM but unable to prevent the release of MSKE in SGM. The protection of ZPG beads with gastro-resistant capsules (Eudragit® L 100-55) resulted in stability in both SGM and SIM; they disintegrated immediately in simulated colonic medium containing pectinolytic enzymes. MSKE-loaded ZPG beads were stable at 4, 25 and 45 °C during the study period of four months. The present study revealed that ZPG beads in enteric-coated capsules might be a promising carrier for delivering MSKE to the colon.
Keywords: colon-targeted delivery; mango seed kernel; calcium-pectinate gel beads; zinc-pectinate gel beads; ionotropic gelation; enteric-coated capsule
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Nithitanakool, S.; Pithayanukul, P.; Bourgeois, S.; Fessi, H.; Bavovada, R. The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract. Molecules 2013, 18, 6504-6520.
Nithitanakool S, Pithayanukul P, Bourgeois S, Fessi H, Bavovada R. The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract. Molecules. 2013; 18(6):6504-6520.
Nithitanakool, Saruth; Pithayanukul, Pimolpan; Bourgeois, Sandrine; Fessi, Hatem; Bavovada, Rapepol. 2013. "The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract." Molecules 18, no. 6: 6504-6520.