Ghosh Debaprasad, Mittal Ashu, Arora Mandeep Kumar
Department of Pharmaceutics, KIET School of Pharmacy, Ghaziabad (Affiliated to Dr. APJ AKTU, Lucknow), Ghaziabad, Uttar Pradesh, India.
Department of Pharmacology, DIT University, Dehradun, Uttarakhand, India.
Drug Dev Ind Pharm. 2025 Oct;51(10):1230-1243. doi: 10.1080/03639045.2025.2525951. Epub 2025 Jul 9.
In this study, we aimed to prepare, evaluate, and compare drug-loaded pellets of ketoprofen coated with different triggering mechanisms for colonic delivery.
The purpose of this study was to compare Eudragit S100 and Eudragit L100 based pH-dependent, hydroxypropyl cellulose and ethyl cellulose-based time-dependent and high methoxylated pectin and ethyl cellulose-based colonic bacterial enzymatic degradation-dependent coatings over drug-loaded pellets for most efficient colon targeting.
Any possible drug-polymer interactions were analyzed using Fourier-transform infrared spectroscopy and differential scanning calorimetry. Drug-loaded pellets were prepared using powder layering technology. Different batches of coated pellets were prepared for evaluation, and optimized batches were selected. These optimized batches were investigated for surface topography by scanning electron microscopy and for colon targeting efficiency by X-ray roentgenography and gamma scintigraphy studies in white New Zealand rabbits.
The drug and polymers were found to be compatible. The prepared coated multi-particulates exhibited favorable micrometric properties. In vitro dissolution studies showed that the polysaccharide pectin high methoxylated and ethyl cellulose-coated optimized batch limited drug release to 16.724 ± 1.124% in the upper gastrointestinal tract and released up to 91.556 ± 3.144% in the colon following zero-order Korsmeyer-peppas super case-II transport (mean dissolution time 36.1779 h). Scanning electron microscopy analysis confirmed the surface characteristics of the pellets before and after dissolution. studies in New Zealand white rabbits using X-ray roentgenography and gamma scintigraphy demonstrated the optimized batch's gastrointestinal transit and colon targeting efficiency.
Statistically, the polysaccharide-based formulation showed promising results for targeted drug release in the colon.
在本研究中，我们旨在制备、评估和比较具有不同触发机制的酮洛芬载药微丸用于结肠给药。
本研究的目的是比较基于Eudragit S100和Eudragit L100的pH依赖性、基于羟丙基纤维素和乙基纤维素的时间依赖性以及基于高甲氧基化果胶和乙基纤维素的结肠细菌酶降解依赖性包衣在载药微丸上的应用，以实现最有效的结肠靶向。
使用傅里叶变换红外光谱和差示扫描量热法分析任何可能的药物 - 聚合物相互作用。采用粉末层积技术制备载药微丸。制备不同批次的包衣微丸进行评估，并选择优化批次。通过扫描电子显微镜研究这些优化批次的表面形貌，并通过X射线造影和γ闪烁显像研究在新西兰白兔中评估结肠靶向效率。
发现药物和聚合物具有相容性。制备的包衣多颗粒具有良好的微观特性。体外溶出研究表明，高甲氧基化多糖果胶和乙基纤维素包衣的优化批次在上消化道将药物释放限制在16.724±1.124%，在结肠中遵循零级Korsmeyer - peppas超Ⅱ型转运释放高达91.556±3.144%（平均溶出时间36.1779小时）。扫描电子显微镜分析证实了溶出前后微丸的表面特征。在新西兰白兔中使用X射线造影和γ闪烁显像的研究证明了优化批次的胃肠道转运和结肠靶向效率。
从统计学角度来看，基于多糖的制剂在结肠靶向药物释放方面显示出有前景的结果。
