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

机译:含泰国芒果籽仁提取物的果胶凝胶珠的研制理化特性和体外释药研究

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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.
机译:开发了含有泰国芒果籽仁提取物(MSKE,品种“ Fahlun”)的果胶凝胶珠,并对其进行了表征,目的是进行结肠靶向递送。负载MSKE的果胶酸盐微珠是通过离子凝胶法制备的,其中离子化凝胶的果胶与MSKE的比例,MSKE浓度以及两种交联剂(氯化钙和醋酸锌)的浓度均不同。配制的珠是球形的,尺寸范围在1.13mm至1.88mm之间。含有大量MSKE的果胶锌(ZPG)珠粒显示MSKE(100%)的完全包封率(EE),而果胶酸钙(CPG)珠粒具有70%EE含量。体外释放测试表明,载有MSKE的CPG珠在模拟胃介质(SGM)和模拟肠介质(SIM)中均不稳定,而载有MSKE的ZPG珠在SIM中稳定,但无法阻止SGM中MSKE的释放。 ZPG珠用耐胃胶囊(Eudragit ® L 100-55)保护可以在SGM和SIM中保持稳定;它们立即在含有果胶分解酶的模拟结肠培养基中崩解。在四个月的研究期内,载有MSKE的ZPG珠在4、25和45°C下稳定。本研究表明,肠溶胶囊中的ZPG珠可能是将MSKE传递至结肠的有希望的载体。

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