Department of Pharmacy, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudthaya Road, Phayathai, Bangkok 10400, Thailand.
Molecules. 2013 Jun 3;18(6):6504-20. doi: 10.3390/molecules18066504.
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.
开发并表征了含有泰国芒果种子仁提取物（MSKE，品种“Fahlun”）的齿状凝胶珠，目的是用于结肠靶向递药。用离子凝胶化法制备载有 MSKE 的果胶珠，改变果胶与 MSKE 的比例、MSKE 浓度和两种交联剂（氯化钙和乙酸锌）的浓度。所制备的珠呈球形，大小在 1.13 毫米至 1.88 毫米之间。含有大量 MSKE 的锌-果胶（ZPG）珠表现出 MSKE 的完全包封效率（EE）（100%），而钙-果胶（CPG）珠的 EE 为 70%。体外释放试验表明，CPG 载 MSKE 珠在模拟胃液（SGM）和模拟肠液（SIM）中均不稳定，而 ZPG 载 MSKE 珠在 SIM 中稳定，但不能防止 MSKE 在 SGM 中的释放。用胃耐胶囊（Eudragit®L 100-55）对 ZPG 珠进行保护，使其在 SGM 和 SIM 中均稳定；它们在含有果胶酶的模拟结肠介质中立即崩解。在四个月的研究期间，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 递送到结肠的有前途的载体。
