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

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 co...

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Autores principales: Nithitanakool, Saruth, Pithayanukul, Pimolpan, Bourgeois, Sandrine, Fessi, Hatem, Bavovada, Rapepol
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270120/
https://www.ncbi.nlm.nih.gov/pubmed/23736787
http://dx.doi.org/10.3390/molecules18066504
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author Nithitanakool, Saruth
Pithayanukul, Pimolpan
Bourgeois, Sandrine
Fessi, Hatem
Bavovada, Rapepol
author_facet Nithitanakool, Saruth
Pithayanukul, Pimolpan
Bourgeois, Sandrine
Fessi, Hatem
Bavovada, Rapepol
author_sort Nithitanakool, Saruth
collection PubMed
description 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.
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spelling pubmed-62701202018-12-17 The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract Nithitanakool, Saruth Pithayanukul, Pimolpan Bourgeois, Sandrine Fessi, Hatem Bavovada, Rapepol Molecules Article 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. MDPI 2013-06-03 /pmc/articles/PMC6270120/ /pubmed/23736787 http://dx.doi.org/10.3390/molecules18066504 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Nithitanakool, Saruth
Pithayanukul, Pimolpan
Bourgeois, Sandrine
Fessi, Hatem
Bavovada, Rapepol
The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract
title The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract
title_full The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract
title_fullStr The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract
title_full_unstemmed The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract
title_short The Development, Physicochemical Characterisation and in Vitro Drug Release Studies of Pectinate Gel Beads Containing Thai Mango Seed Kernel Extract
title_sort development, physicochemical characterisation and in vitro drug release studies of pectinate gel beads containing thai mango seed kernel extract
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270120/
https://www.ncbi.nlm.nih.gov/pubmed/23736787
http://dx.doi.org/10.3390/molecules18066504
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