为显著的抗炎活性而被封闭的柔软体:开发,优化和ex vivo和in vivo评估
Sadek Ahmed1, Diana E Aziz2, Mohamed A Sadek3
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini, Cairo, 11562, Egypt. sadek.sadek@pharma.cu.edu.eg.
Drug delivery and translational research
|February 5, 2024
概括
装有迪亚塞林的柔软体被开发用于治疗骨关节炎,显示改善皮肤透和抗炎作用. 这种新的配方为骨关节炎管理提供了一个有前途的治疗选择,增强了安全性和稳定性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 骨关节炎 (OA) 是一种退行性关节疾病,需要有效的治疗策略.
- 迪亚塞林 (DCN) 是一种具有抗炎性能的 antraquinone 衍生物,但其临床使用受到生物可用性和副作用的限制.
- 柔软体,新型囊泡载体,提供了增强药物输送和治疗结果的潜力.
研究的目的:
- 制定和优化带有白素的柔软体 (DCN-flexosomes) 以提高骨关节炎治疗的疗效.
- 为了研究配方变量对柔性体特征的影响.
- 评估优化DCN-柔性体的物理化学,体内和体外特性.
主要方法:
- 采用2^3的全因数设计,以优化柔性体的配方,不同的表面活性剂类型,度和烯胺量.
- 使用旋转蒸发器准备了柔性体,并以捕获效率 (EE%),泽塔潜力 (ZP),多分散度指数 (PDI) 和颗粒大小 (PS) 进行了表征.
- 进行了全面的物理化学,体内 (透,组织病理学,抗炎,皮肤刺激) 和体外研究.
主要成果:
- 优化的DCN-柔性体配方实现了高可取性 (0.931) 优异的EE% (90.93%),ZP (-40.4 mV) 和小颗粒大小 (188.55 nm).
- 在体内研究表明,与DCN悬浮相比,皮肤透率 (132微米 vs. 48微米) 和沉积率 (193.43微克/厘米2 vs. 66.31微克/厘米2) 显著改善.
- 优化的柔软体表现出增强的抗受体活性 (66%对26%) 和有利的安全性和储存概况.
结论:
- 带有迪亚素的柔软体体代表了一种有前途的先进药物输送系统,用于有效的骨关节炎管理.
- 优化的柔性体显示出优越的治疗潜力,由于增强的透,沉积和抗炎活性.
- 这种配方为治疗骨关节炎提供了一个安全而稳定的替代方案.
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