开发和评估通过人造膜透性的尼亚辛胺通过皮肤的配方
Jeong Sun Sohn1, Jin-Seok Choi2
1College of General Education, Chosun University, PhD, Associate Professor, Gwangju 61452, Republic of Korea.
概括
这项研究开发了一种使用二乙烯糖醇和Tween®80的新型尼亚辛胺 (NAC) 配方,显著提高了通过皮肤递送药物的皮肤透性. 优化的配方在12个月内表现出极好的稳定性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 皮肤病学 皮肤病学
背景情况:
- 皮肤屏障显著阻碍了通过皮肤的药物透性,限制了许多配方的疗效.
- 尼阿辛胺 (NAC) 是生物制药分类系统I类药物,具有高溶解度和肠道透性,但在通过皮肤应用时面临挑战.
- 现有的NAC配方不足以用于先进的输送途径,如通过皮肤或注射.
研究的目的:
- 开发一种具有增强皮肤透性的创新氨胺 (NAC) 配方.
- 确保通过皮肤输送的新型NAC配方的稳定性和安全性.
- 确定最佳的溶剂和透增强剂,以改善NAC的透皮性质.
主要方法:
- 配方开发涉及选择一种溶剂来提高皮肤的透性,其次是透增强剂.
- 在所有开发的配方中,使用人工膜 (Strat-M®) 评估了皮肤的透性.
- 最佳配方 (NF1) 包含NAC/Tween®80 (1:1重量比) 在二乙烯糖醇 (DPG) 中,并在PBS缓冲器 (pH 7.4) 中进行评估.
主要成果:
- 最佳非离子配方 (NF1) 与所有其他测试配方相比,具有最高的皮肤透性.
- NF1显示了变化的热特性,表明配方集成成功.
- 在12个月的稳定期内,NF1保持了稳定的药物含量,外观和pH值.
结论:
- 烯基醇 (DPG) 显著增强了氨胺 (NAC) 通过皮肤的透.
- 在NAC透皮配方中,Tween®80充当了关键的增强剂.
- 开发的创新NAC配方显示了未来人类皮肤间的研究和应用的前景.
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