The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract

Molecules

Saruth Nithitanakool¹  Pimolpan Pithayanukul¹  Sandrine Bourgeois²  Hatem Fessi² 

[1] Department of Pharmacy, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudthaya Road, Phayathai, Bangkok 10400, Thailand; E-Mail:;University Lyon, University Claude-Bernard Lyon 1, LAGEP UMR CNRS 5007, F-69622, Villeurbanne, France; E-Mails:

关键词: colon-targeted delivery;    mango seed kernel;    calcium-pectinate gel beads;    zinc-pectinate gel beads;    ionotropic gelation;    enteric-coated capsule;   

DOI  :  10.3390/molecules18066504

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.