Ghosh Debaprasad, Mittal Ashu, Arora Mandeep Kumar
Department of Pharmaceutics, KIET School of Pharmacy, KIET Group of Institutions, 13 KM Stone, NH 58. Ghaziabad-Meerut Road, Ghaziabad, Uttar Pradesh IN 201206, India.
Department of Pharmaceutics, KIET School of Pharmacy, KIET Group of Institutions, 13 KM stone, NH-58, Ghaziabad-Meerut Road, Ghaziabad, Uttar Pradesh IN 201206, India.
ACS Omega. 2025 Aug 4;10(32):36481-36495. doi: 10.1021/acsomega.5c04979. eCollection 2025 Aug 19.
This study aims to evaluate HM (high methoxyl) pectin from different sources (apple, citrus, and beet) with varying degrees of methyl esterification (DOE) to identify the optimal grade for colonic bacterial enzyme-triggered polymeric coatings for colon-targeted delivery of drugs. Drug-loaded multiparticulates were prepared by a powder layering technique and subsequently coated into distinct trial formulation batches with ethyl cellulose and different HM pectin-based plasticized coating solutions. Otilonium bromide, a model drug for irritable bowel syndrome, was employed. Drug-polymer compatibility was confirmed through FT-IR and DSC studies. The coated multiparticulates demonstrated high drug entrapment efficiency (>85%), favorable micromeritic properties, and minimal loose surface drug crystals (<1.2%). Among the batches, F ( = 0.0042), coated with apple pectin (DOE 50%), exhibited superior colon-targeting efficiency, limiting drug release to 15.47 ± 1.53% under simulated upper gastrointestinal conditions while achieving 78.27 ± 2.11% release under colonic conditions by the ninth hour in vitro Surface topography was analyzed via scanning electron microscopy before and after dissolution. In vivo, X-ray roentgenography, and gamma-scintigraphy studies in New Zealand white rabbits further validated the colon-targeting efficacy of the optimized batch. The source and DOE value of the HM pectin were found to affect premature drug release and colon-targeting efficiency. Apple HM pectin 50% DOE was found to be the ideal HM pectin for microbial enzyme-dependent colon-targeted coatings.
本研究旨在评估来自不同来源（苹果、柑橘和甜菜）、具有不同甲酯化程度（DOE）的高甲氧基（HM）果胶，以确定用于结肠靶向给药的结肠细菌酶触发聚合物包衣的最佳等级。通过粉末分层技术制备载药多颗粒，随后用乙基纤维素和不同的基于HM果胶的增塑包衣溶液将其包衣成不同的试验制剂批次。选用了用于治疗肠易激综合征的模型药物奥替溴铵。通过傅里叶变换红外光谱（FT-IR）和差示扫描量热法（DSC）研究证实了药物与聚合物的相容性。包衣后的多颗粒显示出高药物包封率（>85%）、良好的粉体学性质以及极少的松散表面药物晶体（<1.2%）。在这些批次中，用苹果果胶（DOE 50%）包衣的F批次（=0.0042）表现出卓越的结肠靶向效率，在模拟上胃肠道条件下将药物释放限制在15.47±1.53%，而在结肠条件下到体外第九小时实现了78.27±2.11%的释放。通过扫描电子显微镜在溶解前后分析表面形貌。在新西兰白兔体内进行的X射线透视和γ闪烁扫描研究进一步验证了优化批次的结肠靶向功效。发现HM果胶的来源和DOE值会影响药物的过早释放和结肠靶向效率。发现苹果50% DOE的HM果胶是用于微生物酶依赖性结肠靶向包衣的理想HM果胶。
