在可溶性微针阵列中装载的Costunolide纳米悬浮,用于治疗亚托皮炎
Xulong Xue1, Pengcheng Zhang2, Yang Cao2
1School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, No. 10 Panyanghu Road, Tianjin 301617, China; Military Medical Sciences Academy, Academy of Military Sciences, No. 1 Dali Road, Tianjin 300050, China.
International journal of pharmaceutics
|April 9, 2025
概括
这项研究引入了一种新型的微针系统,用于输送costunolide纳米悬浮剂,改善亚托皮炎治疗的溶解性和生物可用性. 与口服方法相比,通过皮肤治疗的方法显示出更高的疗效和减少炎症.
科学领域:
- 制药科学 制药科学
- 生物材料工程 生物材料工程
- 皮肤病学 皮肤病学
背景情况:
- 传统的口服药物输送面临着水性化合物如costunolide (COS) 的可溶性和生物利用性的局限性.
- 亚托皮炎 (AD) 需要有效的治疗策略,改善药物输送系统.
- 通过皮肤递送药物系统 (TDDS) 提供了一个有希望的替代方案来克服口服的缺点.
研究的目的:
- 开发一种新的通过皮肤递送系统,将costunolide纳米悬浮剂 (COS-NS) 与可溶解微针 (DMN) 结合起来,用于AD治疗.
- 为了提高costunolide的可溶性和生物利用性,以便有效地进行局部应用.
- 在AD小鼠模型中评估COS-NS加载DMN (COS-DMN) 的有效性和安全性.
主要方法:
- 通过抗溶剂沉制备的Costunolide纳米悬浮液 (COS-NS),用PVP K30和SDS稳定,用曼尼托尔冷干燥.
- 将COS-NS纳入基于氨酸的可溶性微针 (DMN) 中,以创建COS-DMN.
- 纳米粒子大小,溶解性,释放动力学,微针机械强度和皮肤透性的表征.
- 在大鼠中进行的药理动力学研究和在2,4-丁二 (DNCB) 诱导的AD小鼠模型中进行的疗效评估.
主要成果:
- 优化的COS-NS纳米粒子 (203.42nm) 显示出增强的溶解度 (388.61μg/mL) 和累积释放率 (93.00%在24小时内).
- COS-DMN 显示出强大的机械强度和高效的皮肤透 (630微米深,95%的成功率).
- 在老鼠中的药理动力学表明,与口服相比,COS-DMN的通过皮肤吸收优于COS-DMN.
- 在AD小鼠中,COS-DMN显著降低了较低剂量的皮肤厚度,和关键炎症类细胞因子 (IgE,TNF-α,IL-13).
结论:
- 开发的COS-DMN系统有效地提高了costunolide的溶解度和通过皮肤传递.
- 在COS-DMN中,COS-DMN为治疗亚托皮性皮肤炎提供了一种微创和高效的治疗策略.
- 这种新的方法提供了一个有前途的平台,可以通过皮肤递送疏水性药物,特别是用于皮肤病.
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