The development, physicochemical characterisation and in vitro drug release studies of pectinate gel beads containing Thai mango seed kernel extract

Molecules. 2013 Jun 3;18(6):6504-20. doi: 10.3390/molecules18066504.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium / chemistry
  • Capsules / chemistry
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • Gels / chemistry
  • Mangifera / chemistry*
  • Microspheres*
  • Particle Size
  • Plant Extracts / chemistry*
  • Seeds / chemistry*
  • Zinc / chemistry

Substances

  • Capsules
  • Drug Carriers
  • Gels
  • Plant Extracts
  • Zinc
  • Calcium