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在体外透试验 (IVPT) 研究中的受体溶液的影响
Minthira Sarnthiratch1, Lama Alsheddi1, Patcharawan Nimmansophon1
1Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH 45267, United States.
Journal of pharmaceutical sciences
|November 16, 2023
概括
在体外透试验 (IVPT) 受体溶液中的添加剂可以提高难以溶解的化学物质的溶解性. 大多数添加剂没有影响皮肤的透性,除了25%的乙醇,这显著增加了它.
科学领域:
- 皮肤和通过皮肤输送药物
- 配方科学科学 配方科学
- 皮肤生理学 皮肤生理学
背景情况:
- 在体外透试验 (IVPT) 对于评估化学物质的皮肤透和皮肤病产品的疗效至关重要.
- 在IVPT受体溶液中提高透溶解性对于不易溶解的化合物至关重要.
- 添加剂用于增加溶解度,而不会损害皮肤屏障的完整性.
研究的目的:
- 评估各种添加剂在IVPT期间对皮肤透性和电阻的影响.
- 为了确定模型透剂在不同受体溶液中的可溶性增强.
- 为了确定适合的添加剂的IVPT的脂性化合物.
主要方法:
- 对含有牛血清白蛋白 (BSA),2-基-β-环极 (HPCD),乙醇,Brij-98和基醇的受体溶液进行比较分析.
- 使用切割皮肤测量稳定状态皮肤透系数.
- 评估皮肤电阻作为屏障功能的指标.
- 在每个受体溶液中确定透溶解度.
主要成果:
- 大多数添加剂 (BSA,HPCD,Brij-98,propylene glycol) 并没有显著改变皮肤的透性或电阻 (<40%的变化).
- 一种含有25%乙醇的受体溶液显著增加了皮肤的透性 (约. 两倍) 和降低电阻 (大约. 这是三倍的).
- 2.5%的HPCD提供了最高的溶解度的脂性透物;0.2%的Brij-98和5%的乙醇显示了与PBS相比最小的溶解度增强.
结论:
- 在IVPT中可以使用受体溶液添加剂,但必须考虑它们对皮肤完整性的影响.
- 25%乙醇显著影响皮肤屏障功能和透性,使其不适合标准IVPT.
- 2.5%的HPCD是一种有希望的选择,可以在IVPT中增强脂性透溶解度,而不会损害皮肤屏障.
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