通过使用Kollidone VA64和Soluplus作为聚合物进行固体分散来增强piperine的溶解性:物理化学表征,分子对接和细胞活力测定
Syed Sarim Imam1, Wael A Mahdi1, Sultan Alshehri1
1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Journal of biomaterials science. Polymer edition
|June 23, 2025
概括
配合Kollidone VA64 (KLD) 和Soluplus (SLP) 的皮佩林 (PRN) 的三级固体分散显著提高了PRN的溶解性和溶解率. 与二进制系统和自由PRN相比,这些piperine固体分散也改善了药物释放和细胞活力.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 皮佩林 (PRN) 是一种水溶性较差的化物,具有多样化的生物活性.
- 提高PRN的可溶性和生物利用性对于其治疗应用至关重要.
- 固体分散 (SDs) 提供了一个有前途的策略来克服药物溶解性差.
研究的目的:
- 开发和描述使用Kollidone VA64 (KLD) 和Soluplus (SLP) 作为载体的piperine固体分散物 (PRN SD).
- 为了提高piperine的可溶性,溶解率和生物可用性.
- 评估开发的SDs的药物聚合物兼容性,结晶性和体外疗效.
主要方法:
- 阶段溶解性研究以确定稳定常数.
- 溶解和和可溶性研究以优化成分.
- 红外 (IR) 和核磁共振 (NMR) 光谱用于兼容性评估.
- 扫描电子显微镜 (SEM) 和X射线衍射 (XRD) 用于结晶性分析.
- 在乳腺癌细胞系上进行细胞活力测试.
主要成果:
- 三元PRN-KLD-SLP系统的稳定常数明显高于二元系统.
- 与二进制SD和自由PRN相比,三进制PRNSD显示药物释放的1.4倍增强.
- 光谱分析和分子对接证实了稳定的SD形成.
- SEM和XRD表示晶体PRN转换为无形形式.
- 细胞活力测定表明PRN从三元SDs的有效性得到改善.
结论:
- 三级固体分散配方是一种有效的方法来增强piperine的溶解性和溶解性.
- 开发的三元PRN SD表现出优越的性能比二元系统和免费piperine.
- 无形转换和改善药物释放有助于增强皮佩林的治疗潜力.
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