Design, Formulation and Characterization of Microspheres containing Mesalamine for the Treatment of Ulcerative Colitis

Deepa H. Patel, S. Shah, C. Tyagi
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引用次数: 1

Abstract

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72% - 82.27%, drug loading from 20.28% - 33.26%. The size of the prepared microspheres ranged between 61.22-90.41μm which was found to increase with increase in polymer concentration. All values are statistically significant as p<0.05. The release profile of mesalamine from eudragit-coated chitosan micro-spheres was found to be pH dependent. It was observed that Eudragit S100 coated chitosan microspheres gave no release in the simulated gastric fluid, negligible release in the simulated intestinal fluid and maximum release in the colonic environment. It was concluded from the study that Eudragit-coated chitosan microspheres were promising carriers for colon-targeted delivery of Mesalamine.
治疗溃疡性结肠炎的美沙拉胺微球的设计、配方和表征
本研究的目的是制备,表征和评价结肠靶向美沙拉胺微球治疗和管理溃疡性结肠炎(UC)。以三聚磷酸盐(TPP)为交联剂,采用离子凝胶乳化法制备微球。采用溶剂蒸发技术在微球表面包被乌龙茶S-100,以防止药物在胃内释放。对制备的微球进行了表面形貌、包封效率、载药量、微粒学性能和体外释药性能的评价。在扫描电子显微镜下观察到形成的微球表面粗糙。微球的包封效率为43.72% ~ 82.27%,载药量为20.28% ~ 33.26%。制备的微球粒径在61.22 ~ 90.41μm之间,随聚合物浓度的增加而增大。p<0.05,差异有统计学意义。结果表明,壳聚糖微球对美沙拉胺的释放具有pH依赖性。结果表明,壳聚糖微球在模拟胃液中无释放,在模拟肠液中释放量可忽略,在结肠环境中释放量最大。研究结果表明,桉木聚糖包被壳聚糖微球是一种很有前途的美沙拉胺结肠靶向递送载体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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