title: The development, physicochemical characterisation and in vitro drug release studies of pectinate gel beads containing Thai mango seed kernel extract.
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.
authors.affiliation: Department of Pharmacy, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudthaya Road, Phayathai, Bangkok 10400, Thailand. saruth_pipe@yahoo.com
authors.forename: Saruth
authors.initials: S
authors.lastname: Nithitanakool
authors.forename: Pimolpan
authors.initials: P
authors.lastname: Pithayanukul
authors.forename: Sandrine
authors.initials: S
authors.lastname: Bourgeois
authors.forename: Hatem
authors.initials: H
authors.lastname: Fessi
authors.forename: Rapepol
authors.initials: R
authors.lastname: Bavovada
mesh_terms: D002118:Calcium / Q000737:chemistry; D002214:Capsules / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005782:Gels / Q000737:chemistry; D031022:Mangifera / Q000737:chemistry*; D008863:Microspheres; D010316:Particle Size; D010936:Plant Extracts / Q000737:chemistry*; D012639:Seeds / Q000737:chemistry*; D015032:Zinc / Q000737:chemistry
chemical_list: D002214:Capsules; D004337:Drug Carriers; D005782:Gels; D010936:Plant Extracts; D015032:Zinc; D002118:Calcium