快速溶解的微针贴片与贝尼迪平荷载纳米转移体集成,用于通过皮肤递送药物:优化,表征和临床前生物可用性评估
Khater Al-Japairai1, Samah Hamed Almurisi2, Fawaz Alheibshy3
1Department of Pharmaceutical Engineering, Faculty of Chemical and Process Engineering Technology, Universiti Malaysia Pahang Al-Sultan Abdullah, 26300, Gambang, Malaysia.
Drug delivery and translational research
|October 15, 2025
概括
这项研究开发了一种新型的通过皮肤贴片,使用贝尼迪平化 (BEN) 载荷纳米转移体 (BEN-TF) 溶解微针 (DMN). 与口服相比,这种方法显著提高了BEN的生物可用性.
科学领域:
- 制药科学 制药科学
- 生物材料工程 生物材料工程
- 药物输送系统 药物输送系统
背景情况:
- 高血压管理通常依赖于贝尼迪平化 (BEN),但由于口服生物可用性较低,其有效性受到阻碍.
- 通过皮肤递送药物提供了一种替代途径,以克服口服生物可用性限制.
研究的目的:
- 开发和评估一种新型的杂性贝尼迪平化 (BEN) 通过皮肤递送系统.
- 通过纳米转移体集成到溶解微针 (DMN) 中,增强BEN的全身传递和生物可用性.
主要方法:
- 使用Box-Behnken设计和薄膜水化,优化带有BEN的纳米转移体 (BEN-TF).
- 描述 BEN-TF 的物理化学特性 (大小,捕获效率,形态) 和药物状态 (DSC,ATR-FTIR,XRD).
- 制造和评估BEN-TF装载溶解微针 (BEN-TF-DMNs),包括皮肤透 (聚焦显微镜),ex-vivo透和in-vivo生物利用性研究.
主要成果:
- 优化的BEN-TF表现出124.9nm的囊泡大小,高捕获效率 (98.12%) 和显著的皮肤间流量 (9.74μg/cm2/hr).
- 证实BEN在配方中处于无形状态.
- 与单独的口服BEN和BEN-DMN相比,BEN-TF-DMN表现出高效的皮肤插入,快速溶解,优异的活体透和活体生物利用性.
结论:
- 开发的BEN-TF-DMNs混合系统有效地克服了BEN.的口服生物可用性较差.
- 这种创新的透皮平台显示出显著的潜力,可以改善贝尼迪平化在高血压管理中的全身输送和治疗疗效.
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