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含泰国芒果种子仁提取物的果胶凝胶珠的研制、理化性质表征及体外药物释放研究。

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

机构信息

Department of Pharmacy, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudthaya Road, Phayathai, Bangkok 10400, Thailand.

出版信息

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3538/6270120/f6ce6377bee8/molecules-18-06504-g001.jpg

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