Khamkar Pruthvi P, Wagh Kalpeshkumar S, Nangare Sopan N, Mali Sachin S, Patil Gaurav S
Department of Pharmaceutics, KVPS's, Institute of Pharmaceutical Education, 425428 Boradi, Maharashtra, India.
Department of Pharmaceutics, Krishna Institute of Pharmacy, Krishna Vishwa Vidyapeeth, 415539 Karad, Maharashtra, India.
Ann Pharm Fr. 2025 May;83(3):514-528. doi: 10.1016/j.pharma.2024.11.006. Epub 2024 Nov 29.
Mesalamine (MES) is a preferred therapeutic agent for managing various colon disorders, including inflammatory bowel diseases (IBD). However, conventional oral dosage forms of MES face significant limitations, which reduce their effectiveness in managing these conditions. To overcome these challenges, advanced dosage forms of MES are essential. Fenugreek gum (FG), a natural polysaccharide with non-toxicity, ease of synthesis, biodegradability, and biocompatibility, was selected as a key component for developing a novel delivery system. Calcium ion crosslinked MES-incorporated FG-decorated pectin microspheres (FG@MES/PM) were successfully designed for colon-specific drug delivery using an ionotropic gelation technique. The microspheres exhibited favorable physicochemical characteristics, including a particle size of 586nm, a polydispersity index of 0.348, an entrapment efficiency of 85.20±1.02%, and a drug content of 98.52±0.96%. Ex vivo mucoadhesion tests demonstrated strong mucoadhesive properties, highlighting the potential of FG@MES/PM to adhere effectively to the colonic mucosa. In vitro drug release studies showed a modified release profile, with 99.02±1.80% MES released over 24h. Release kinetics analysis confirmed that FG@MES/PM followed the Higuchi matrix model (R=0.9867), indicating diffusion-controlled release. The drug release mechanism was characterized as anomalous (non-Fickian) transport, with a release exponent (n) of 0.563. Overall, FG@MES/PM demonstrated promising potential for colon-specific drug delivery, offering sustained release and enhanced mucoadhesion. This study underscores the utility of FG for developing advanced drug delivery systems targeting the colon. Future research should explore the broader application of FG and similar natural polysaccharides in designing efficient and biocompatible colon-targeted formulations to improve therapeutic outcomes for IBD and related conditions.
美沙拉嗪（MES）是治疗各种结肠疾病（包括炎症性肠病（IBD））的首选治疗药物。然而，MES的传统口服剂型存在显著局限性，这降低了它们在治疗这些疾病中的有效性。为了克服这些挑战，开发先进的MES剂型至关重要。胡芦巴胶（FG）是一种天然多糖，具有无毒、易于合成、可生物降解和生物相容性等特点，被选为开发新型给药系统的关键成分。采用离子凝胶技术成功设计了钙离子交联的载MES的FG修饰果胶微球（FG@MES/PM）用于结肠特异性药物递送。微球表现出良好的物理化学特性，包括粒径为586nm、多分散指数为0.348、包封率为85.20±1.02%以及药物含量为98.52±0.96%。体外黏膜黏附试验表明其具有很强的黏膜黏附特性，突出了FG@MES/PM有效黏附于结肠黏膜的潜力。体外药物释放研究显示出缓释曲线，24小时内释放了99.02±1.80%的MES。释放动力学分析证实FG@MES/PM符合Higuchi基质模型（R=0.9867）,表明为扩散控制释放。药物释放机制的特征为非Fickian转运，释放指数（n）为0.563。总体而言，FG@MES/PM在结肠特异性药物递送方面显示出有前景的潜力，具有缓释和增强的黏膜黏附性。本研究强调了FG在开发靶向结肠的先进药物递送系统中的实用性。未来的研究应探索FG和类似天然多糖在设计高效且生物相容的结肠靶向制剂中的更广泛应用，以改善IBD及相关病症的治疗效果。
