通过使用实验设计的湿方法开发皮肤里多卡因纳米悬浮配方:体外/体外评估
Özlem Kral1,2, Sibel Ilbasmis-Tamer1, Sevtap Han3
1Department of Pharmaceutical Technology, Gazi University, Ankara 06560, Turkey.
ACS omega
|January 6, 2025
概括
这项研究开发了利多卡因 (LID) 纳米悬浮剂,用于增强皮肤输送. 与传统的LID悬浮相比,纳米悬浮配方显著改善了皮肤积累和镇痛效果.
科学领域:
- 制药科学 制药科学
- 纳米技术纳米技术
- 皮肤药物输送 皮肤药物输送
背景情况:
- 利多卡因 (LID) 是一种广泛使用的局部麻醉剂,具有较差的水溶性,限制了其皮肤应用的有效性.
- 纳米化提供了一种策略,可以提高LID.等难溶药物的可溶性,溶解率和生物可用性.
研究的目的:
- 开发和描述使用湿媒体磨粉方法的利多卡因纳米悬浮剂.
- 评估纳米化对LID皮肤生物可用性,皮肤透性和止痛作用的影响.
- 探索设计实验 (DOE) 在优化纳米悬浮配方中的实用性.
主要方法:
- 通过使用波洛克萨默 (POL) 或聚乙醇 (PVA) 作为稳定剂的湿媒磨,制备了LID的纳米悬浮.
- 鉴定包括粒子大小,多分散度指数,泽塔潜力,DSC,FTIR,XRD和SEM.
- 进行了体外释放,体外皮肤透和体内 analgesic (尾巴试验) 的研究.
主要成果:
- 优化的纳米悬浮实现了低于300nm的粒子大小,具有良好的稳定性 (PDI <0.5,ZP <-20mV).
- 与粗LID悬浮相比,POL/LID和PVA/LID纳米悬浮显示出大约1.8倍的皮肤积累.
- 在体内研究表明,纳米悬浮配方具有统计学上优异的止痛作用.
结论:
- 利多卡因纳米悬浮剂显著提高皮肤生物可用性和止痛功效.
- 湿媒削是LID纳米悬浮制剂的有效方法,POL是合适的稳定剂.
- 能源部是优化纳米悬浮开发流程的宝贵工具.
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