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纤维素 ω-carboxythioalkyl alkanoate衍生物的设计和合成,用于疏水化合物的无形固体分散

Sara Yazdi¹, Emily Benson², Lynne S Taylor²

¹Department of Sustainable Biomaterials, Virginia Tech, 230 Cheatham Hall, Blacksburg, Virginia, 24061, United States; Macromolecules Innovation Institute, Virginia Tech, Blacksburg, Virginia, 24061, United States.

Carbohydrate polymers

|November 30, 2025

概括

新型纤维素衍生物被合成,以改善口服药物输送. 这些无形固体分散 (ASD) 增强了药物的溶解性和生物可用性,其性能与商业聚合物相当.

科学领域:

材料科学材料科学材料科学
聚合物化学聚合物化学
制药科学制药科学

背景情况:

许多药物由于其晶体和疏水性质,具有较差的水溶性,限制了口服生物可用性.
无形固体分散 (ASD) 是一种通过在聚合物矩阵内分散药物分子来增强药物溶解性的策略.
现有的商业ASD聚合物并没有专门为此应用而设计,有时会导致配方失败.

研究的目的:

设计,合成和评估新型 ω-carboxy-thioalkyl纤维素衍生物作为无形固体分散 (ASD) 的聚合物.
研究这些新型聚合物的潜力,以提高难溶性药物的可溶性和生物可用性.

主要方法:

通过区域选择性C6化合成纤维素酸 (CA) 衍生物,然后用功能性硫醇取代硫醇.
在纤维素骨干中加入疏水性侧链和疏水性碳酸盐群.
使用模型药物进行ASD表现的体外评估,评估药物释放和药物-聚合物相互作用.

主要成果:

合成的 ω-carboxy-thioalkyl纤维素衍生物的ASD性能与领先的商业聚合物相美.
对于含有酸性聚合物的基本药物,观察到药物聚合物复合,影响药物释放.
修改聚合物的水友性和使用重的对面层成功地减轻了药物-聚合物复杂化,并改善了释放.

结论:

新型纤维素衍生物显示出作为有效的ASD聚合物来增强疏水药物的可溶性.
了解和减轻药物聚合物相互作用对于优化ASD性能至关重要,特别是对于基本药物.
这些量身定制的纤维素衍生物为开发先进的口服药物输送系统提供了商业聚合物的可行替代品.

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