伊特拉科纳装载纳米乳液:汉森溶解度和电荷驱动的透和基于GastroPlus的预测体内性能
Afzal Hussain1, Mohammad A Altamimi1, Mudassar Shahid1
1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
概括
与传统悬浮剂相比,阴离子纳米乳液显著提高了口服伊特拉科纳 (ITZ) 的吸收. 这项研究利用计算建模和体外数据来预测和确认改善药物透率和治疗系统性真菌感染的疗效.
科学领域:
- 药理学 药理学是指药理学的学科.
- 纳米技术纳米技术
- 计算建模 计算建模
背景情况:
- 有限的体内数据存在于口服伊特拉科纳 (ITZ) 透从阴离子纳米乳液.
- 开发有效的口服药物输送系统对于治疗全身真菌感染至关重要.
研究的目的:
- 在口服后研究ITZ加载的阴离子纳米乳液 (MCNE11) 的体内透概况.
- 通过计算和体外实验方法,比较纳米乳液与口服悬浮剂的性能.
主要方法:
- 使用HSPiP和GastroPlus的ITZ装载纳米乳液 (MCNE11,MNE11) 的配方.
- 使用GastroPlus进行体外溶解研究和体内性能模拟.
- 同焦激光扫描显微镜 (CLSM) 评估粘膜透.
- 参数灵敏度分析 (PSA) 和区域吸收区建模.
主要成果:
- GastroPlus的模拟预测 MCNE11 的药物释放率为 100%,而 12 小时悬停的药物释放率为 32% (pH 6.8).
- 与悬浮剂 (1.5 × 10^-2 μg/mL) 相比,MCNE11的血度显著更高 (1.9 × 10^2 μg/mL).
- 通过纳米乳液载体,CLSM证实了增强的ITZ吸收,支持Fickian扩散 (韦布尔模型,β < 0.75).
结论:
- 与悬浮剂相比,阴离子纳米乳液 (MCNE11) 显示ITZ的口服吸收优于悬浮剂.
- 计算建模 (HSPiP,GastroPlus) 能够有效地预测体内药物性能.
- 基于纳米乳液的输送最大限度地提高了ITZ吸收,用于潜在的全身真菌感染治疗.
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