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树胶作为一种新型生物聚合物用于pH敏感药物递送中的微珠制剂。

gum as a novel biopolymer for microbead formulation in pH-sensitive drug delivery.

作者信息

Basharat Maryam, Noreen Sobia, Khan Amjid, Anwar Farooq, Ijaz Bushra, Munawar Khurram Shahzad, Anwar Mudeera, Abdullah M

机构信息

Institute of Chemistry, University of Sargodha, Sargodha, Pakistan.

Department of Plant Sciences, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.

出版信息

Drug Dev Ind Pharm. 2025 Jul 15:1-19. doi: 10.1080/03639045.2025.2531402.

DOI:10.1080/03639045.2025.2531402
PMID:40650502
Abstract

OBJECTIVE

Biocompatible drug delivery systems that endure stomach acidity while enabling controlled release in the colon are essential for enhancing bioavailability.

SIGNIFICANCE

This study presents () gum, a plant-based substitute for synthetic excipients and a natural, biodegradable polymer for controlled drug delivery. It helps create safer, more efficient oral formulations with more stability of acid-labile drugs.

METHOD

gum was utilized to create plain, blended ( gum and sodium alginate were used in a blended formulation to increase stability, drug entrapment, and controlled release), and coated (Propylene glycol and gum mixture was used as the coating material) microbeads the ionic gelation method.

RESULT

Characterization showed that the size of plain microbeads was 645.67 ± 7.74 μm, while the size of coated microbeads was 586.23 ± 7.18 μm. Drug entrapment efficiency ranged from 67.06% to 88.12%. Swelling studies in pH 7.4 buffer revealed that coated microbeads had a higher swelling index (1.47 ± 0.09) than blended microbeads (1.18 ± 0.06). release studies demonstrated sustained release, as predicted by the Korsmeyer-Peppas model, indicating non-Fickian diffusion. Scanning Electron Microscopy (SEM) results revealed spherical microbeads with varying surface morphologies, including rough, porous, and smooth textures, depending on the formulation. Thermogravimetric Analysis (TGA) and Differential Scanning Calorimetry (DSC) confirm the stability of microbeads. Powder X-ray Diffraction (PXRD) confirmed the amorphous form of P-Na within the microbeads, and Fourier-Transform Infrared Spectroscopy (FTIR) validated successful drug entrapment without significant interactions with the polymer. Acute toxicity studies on Swiss albino mice showed no adverse effects, and pharmacokinetic studies in rabbits demonstrated a prolonged P-Na half-life, increasing from 1.12 to 2.24 hrs with a C of 2264.8 ng/mL.

CONCLUSION

These findings suggest that gum-based microbeads are promising candidates for sustained drug delivery applications. Future research should focus on optimizing these formulations for various drugs, exploring additional therapeutic applications, and investigating the long-term stability of gum-based systems for potential clinical use.

摘要

目的

生物相容性药物递送系统能够耐受胃酸,同时实现结肠中的控释,这对于提高生物利用度至关重要。

意义

本研究展示了()胶,一种基于植物的合成赋形剂替代品,以及一种用于控释药物递送的天然可生物降解聚合物。它有助于创建更安全、更高效的口服制剂,提高酸不稳定药物的稳定性。

方法

利用()胶通过离子凝胶法制备普通微珠、混合微珠(将()胶和海藻酸钠用于混合制剂以提高稳定性、药物包封率和控释效果)和包衣微珠(丙二醇和()胶混合物用作包衣材料)。

结果

表征显示普通微珠的尺寸为645.67±7.74μm,而包衣微珠的尺寸为586.23±7.18μm。药物包封率在67.06%至88.12%之间。在pH 7.4缓冲液中的溶胀研究表明,包衣微珠的溶胀指数(1.47±0.09)高于混合微珠(1.18±0.06)。释放研究表明药物呈持续释放,如Korsmeyer-Peppas模型所预测,表明为非Fickian扩散。扫描电子显微镜(SEM)结果显示微珠呈球形,表面形态各异,包括粗糙、多孔和光滑的纹理,这取决于制剂类型。热重分析(TGA)和差示扫描量热法(DSC)证实了微珠的稳定性。粉末X射线衍射(PXRD)证实微珠内P-Na为无定形形式,傅里叶变换红外光谱(FTIR)验证了药物成功包封且与聚合物无显著相互作用。对瑞士白化小鼠的急性毒性研究未显示不良反应 在兔子身上进行的()胶药代动力学研究表明,P-Na半衰期延长,从1.12小时增至2.24小时,Cmax为2264.8 ng/mL。

结论

这些发现表明基于()胶的微珠有望用于持续药物递送应用。未来的研究应集中于针对各种药物优化这些制剂、探索更多治疗应用,以及研究基于()胶的系统用于潜在临床应用时的长期稳定性。

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