Amidated xanthan gum-coated gastroretentive beads for controlled release of chebulinic acid solid dispersions

IF 2.4 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research Pub Date : 2025-05-19 DOI:10.1016/j.carres.2025.109528

Bigul Yogeshver Bhardwaj , Uma Ranjan Lal , Ram Prakash Dwivedi , Jen Chang Yang , Poonam Negi

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Abstract

This study investigates the usefulness of chemically modified xanthan gum (XG), a natural polysaccharide known for its mucoadhesive and swelling characteristics, in gastroretentive drug delivery systems. XG was modified through amidation using triethanolamine in the presence of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC) as a coupling agent. The resulting amidated xanthan gum (AXG) exhibited significantly improved physicochemical properties, including reduced hydrophilicity, enhanced thermal stability, and increased crystallinity, as confirmed by FTIR, DSC, XRD, and ^1H NMR analyses. Sodium alginate beads were prepared via the ionotropic gelation and subsequently coated with XG and AXG through diffusion-controlled interfacial complexation. The formulations demonstrated sustained drug release (74.8–93.1 %), low densities (0.524–0.40 g/cm³), minimal lag time (5.12–6.18 s), and high drug encapsulation efficiency (58.01–66.43 %). AXG-coated formulations exhibited a higher swelling index (161 %) compared to XG-coated formulations (119 %). SEM analysis revealed the presence of AXG fragments on the bead surfaces. Ex vivo studies confirmed superior mucoadhesive properties of AXG (58 %) compared to XG (46 %). In conclusion, AXG-based composites outperformed XG in achieving targeted and controlled drug delivery to the stomach.

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改良黄原胶包被胃保留珠用于控制释放盐酸固体分散体

本研究探讨了化学改性黄原胶（XG）在胃保留性药物传递系统中的用途，黄原胶是一种天然多糖，以其黏附和肿胀特性而闻名。以1-乙基-3-（3-二甲氨基丙基）碳二亚胺（EDC）为偶联剂，利用三乙醇胺对XG进行酰胺化改性。经FTIR、DSC、XRD和^1H NMR分析证实，改性黄原胶（AXG）的理化性质得到了显著改善，包括亲水性降低、热稳定性增强和结晶度增加。通过离子化凝胶法制备海藻酸钠微球，并通过扩散控制界面络合作用包被XG和AXG。该制剂具有缓释（74.8 ~ 93.1%）、低密度（0.524 ~ 0.40 g/cm3）、最小延迟时间（5.12 ~ 6.18 s）、高包封率（58.01 ~ 66.43%）等特点。与xg包覆制剂（119%）相比，axg包覆制剂表现出更高的膨胀指数（161%）。扫描电镜分析显示，在头表面存在AXG碎片。体外研究证实，与XG（46%）相比，AXG（58%）具有更好的黏附性能。综上所述，基于axg的复合材料在实现胃靶向和控制药物递送方面优于XG。

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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来源期刊

Carbohydrate Research 化学-生化与分子生物学

CiteScore

5.00

自引率

3.20%

发文量

183

审稿时长

3.6 weeks

期刊介绍： Carbohydrate Research publishes reports of original research in the following areas of carbohydrate science: action of enzymes, analytical chemistry, biochemistry (biosynthesis, degradation, structural and functional biochemistry, conformation, molecular recognition, enzyme mechanisms, carbohydrate-processing enzymes, including glycosidases and glycosyltransferases), chemical synthesis, isolation of natural products, physicochemical studies, reactions and their mechanisms, the study of structures and stereochemistry, and technological aspects. Papers on polysaccharides should have a "molecular" component; that is a paper on new or modified polysaccharides should include structural information and characterization in addition to the usual studies of rheological properties and the like. A paper on a new, naturally occurring polysaccharide should include structural information, defining monosaccharide components and linkage sequence. Papers devoted wholly or partly to X-ray crystallographic studies, or to computational aspects (molecular mechanics or molecular orbital calculations, simulations via molecular dynamics), will be considered if they meet certain criteria. For computational papers the requirements are that the methods used be specified in sufficient detail to permit replication of the results, and that the conclusions be shown to have relevance to experimental observations - the authors'' own data or data from the literature. Specific directions for the presentation of X-ray data are given below under Results and "discussion".