通过将其纳入循环德克斯特林中,改善了脂质体托索夫洛克萨的封装和潜力
Hemat Mostafa1, Hamid Alghurabi2, Koki Ogawa1
1Drug Delivery and Nano Pharmaceutics, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-Dori, Mizuho-Ku, Nagoya, 467-8603, Japan.
AAPS PharmSciTech
|November 20, 2025
概括
propyl-β-cyclodextrin (HP-β-CD) 复合物显著提高了tosofloxacin (TFLX) 的溶解性和脂质体封装效率. 这种双交付系统增强了TFLX的功能.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 抗菌剂 抗菌剂 抗菌剂
背景情况:
- 脂质体配方和内输送是提高抗微生物药物的疗效的先进策略.
- 托苏夫洛克萨 (TFLX) 是一种强效的诺,在使用常规方法的脂质体中表现出较差的水溶性和低封装效率 (EE).
- 解决这些局限性对于优化TFLX治疗潜力至关重要.
研究的目的:
- 通过使用xypropyl-β-cyclodextrin (HP-β-CD) 来改善托苏夫洛克萨 (TFLX) 的溶解性和脂质体负荷.
- 开发和表征一种新的TFLX/HP-β-CD脂质体配方,用于增强抗菌剂的输送.
- 评估开发的配方的物理化学性质,药物释放动力学和细胞内抗菌疗效.
主要方法:
- 通过相位溶解性分析优化TFLX/HP-β-CD纳入复合物的准备.
- 使用薄膜水化方法将TFLX/HP-β-CD复合物纳入脂质体.
- 使用里埃变换红外光谱 (FTIR) 和X射线衍射 (XRD) 的表征,同时评估封装效率,体外药物释放和细胞内抗菌活性,对黄金葡萄球菌.
主要成果:
- 惠普-β-CD复合增加了TFLX溶解度约25倍.
- 与传统的TFLX-脂质体 (17.9%) 相比,TFLX/HP-β-CD脂质体表现出明显更高的EE (69.7%).
- 该配方在48小时内表现出持续的药物释放,以及对黄金葡萄球菌 (Staphylococcus aureus) 的优越细胞内抗菌疗效.
结论:
- 结合HP-β-CD复合和脂质体封装,有效地提高TFLX溶解性,加载效率和细胞内抗菌活性.
- FTIR和XRD分析证实了TFLX/HP-β-CD纳入复合物的形成.
- 这种双交付策略为制备水溶性较差的抗微生物剂提供了一个有前途的平台,特别是用于肺部的输送.
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