含有黄素的soluplus®三元固体分散剂,具有增强的溶解性,溶解性和抗菌,抗氧化,抗炎作用
Memoona Ishtiaq1, Hina Manzoor2, Ikram Ullah Khan1
1Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad 38000, Pakistan.
三级无形固体分散 (ASDs) 显著增强黄素.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 无形固体分散 (ASD) 对于提高药物的溶解性和生物可用性至关重要.
- 二元ASD系统通常显示有限的长期溶解性,需要先进的配方.
研究的目的:
- 设计和评估黄素 (CUR) 的三元形态无形固体分散 (TSD).
- 提高黄素的溶解性,溶解率和生物活性 (抗菌,抗氧化,抗炎).
主要方法:
- 使用Soluplus®,Syloid® XDP 3150,Syloid® 244,Poloxamer® 188和HPMC E5通过溶剂蒸发来制备TSD.
- 可溶性和溶解性测试. 溶解性和溶解性测试.
- 使用FTIR,SEM,DSC和XRD进行固态表征.
- 在体外评估抗菌,抗氧化和抗炎活性.
主要成果:
- 含有20%Soluplus®的优化三元制剂 (F3) 显著增加了黄素的溶解性 (186μg/ml) 和溶解 (91%),分别增加了3100倍和9倍.
- 固态分析证实了TSD的无形性质和增强性质.
- 在F3的抗菌活性显著改善,对抗格拉姆阳性和格拉姆阴性细菌,特别是对抗金黄色葡萄球菌 (24毫米抑制区域).
- 抗氧化活性增加到93% (相对于CUR的69%),而抗炎活性显示80%的BSA抑制 (相对于CUR的49%).
结论:
- 三级无形固体分散,特别是F3,是提高黄素可溶性和溶解性的高效系统.
- 与纯黄相比,开发的TSD表现出优越的抗菌,抗氧化和抗炎性质.
- 这种配方策略有望改善黄素等疏水药物的输送和疗效.
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