Formulation and evaluation of hydrocortisone micro beads

Khaja Moinuddin Shaik, Pradeep Kumar M, Jagadeesh Babu B, Manjula C
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Abstract

The current study aimed to develop hydrocortisone mucoadhesive microbeads to prolong the drug's action in the gastrointestinal system, targeting Crohn's disease treatment. Hydrocortisone, known for its anti-inflammatory and anti-rheumatic effects, was utilized in bead form to enhance therapeutic efficacy, extend residence time, and reduce dosage frequency. Using sodium alginate, HPMC, and Eudragit L-100 as adhesive polymers, and calcium chloride and aluminium chloride as cross-linking agents, the study crafted microbeads with an entrapment efficiency between 57.23% and 91.69%. Evaluations focused on in vitro drug release, particle size, surface characteristics, entrapment efficiency, and the role of cross-linking ions. Of the formulations, HCS-8 (with sodium alginate and Eudragit L-100 using aluminium chloride as the gelling solution) and HCS-2 showed optimal drug release profiles. Notably, HCS-8 achieved a 12-hour drug release delay, attributed to aluminium chloride's cross-linking action. Drug release kinetics revealed a zero-order linearity (R2=0.99), suggesting super case 2 transport as the primary release mechanism.
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氢化可的松微珠的配制和评估
本研究旨在开发氢化可的松粘液微珠,以延长药物在胃肠道系统中的作用时间,从而达到治疗克罗恩病的目的。氢化可的松以其抗炎和抗风湿作用而闻名,以微珠形式使用可提高疗效、延长停留时间并减少用药次数。该研究使用海藻酸钠、HPMC 和 Eudragit L-100 作为粘合聚合物,氯化钙和氯化铝作为交联剂,制成了夹持效率在 57.23% 到 91.69% 之间的微珠。评价的重点是体外药物释放、粒度、表面特征、夹持效率和交联离子的作用。在这些制剂中,HCS-8(海藻酸钠和 Eudragit L-100,使用氯化铝作为胶凝溶液)和 HCS-2 显示出最佳的药物释放曲线。值得注意的是,HCS-8 实现了 12 小时的药物释放延迟,这归功于氯化铝的交联作用。药物释放动力学显示出零阶线性关系(R2=0.99),表明超情况 2 运输是主要的释放机制。
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