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在脂基药物配方中的油阶段中,水性深性溶剂 (HDES)

Shaida Panbachi¹, Josef Beranek², Martin Kuentz³

¹Zentiva, k.s., U Kabelovny 130 102 00, Praha 10, Czech Republic; University of Basel, Department of Pharmaceutical Sciences, Klingelbergstrasse 50 4056, Basel, Switzerland; University of Applied Sciences and Arts Northwest. Switzerland, School of Life Sciences, Institute of Pharma Technology, Hofackerstr. 30 CH- 4132, Muttenz, Switzerland.

International journal of pharmaceutics

|July 4, 2024

概括

这项研究引入了一种新型的疏水性深度浸泡溶剂 (HDES),用于增强药物输送配方. 将HDES与表面活性剂结合起来可以改善药物的溶解和释放,为基于脂质的配方提供了一个有前途的新方法.

科学领域:

制药科学制药科学
材料科学材料科学材料科学
物理化学物理化学

背景情况:

深度环氧溶剂 (DES) 正在成为制药制造和药物输送中的绿色替代品.
基于脂质的配方 (LBF) 对于提供疏水性药物至关重要.
在LBF中,水性DES尚未得到广泛的探索.

研究的目的:

为了研究一种新型的疏水性深溶剂 (HDES),用于基于脂质的药物输送.
描述HDES的相位行为和药物溶解能力.
评估HDES与表面活性剂相结合的潜力,以改善药物输送.

主要方法:

一种酸:多德酸混合物 (2:1M比率) 的实验阶段行为研究.
对HDES的热力学建模.
用一种疏水性模型药物 (Venetoclax) 对HDES进行原子分子动力学模拟.
在HDES中对药物溶解的评估与传统车辆相比.
评估水性分散和体外药物释放,有或没有表面活性剂 (Tween 80).

主要成果:

与传统的基于糖的车辆相比,HDES显示了疏水药物Venetoclax的显著增强溶解.
HDES最初的水性分散是有限的.
添加Tween 80改善了分散,导致更小的水滴大小和高的体外药物释放.
分子动力学模拟为HDES中的组件相互作用提供了洞察力.

结论:

HDES与表面活性剂的组合代表了一种新的,有前途的基于脂质的配方,具有很高的制药潜力.
谨慎平衡HDES和表面活性成分是保持HDES完整性的关键,同时确保适当的分散和药物释放.
这种方法为使用绿色溶剂技术制备疏水药物提供了新的途径.

关键词:

先进的配方 (s)深层欧性溶剂 (s)欧特克学 (Eutectic) 是一个学科.基于脂质的配方 (((s)新型药物 (新型药物)难溶的药物 (s) 难溶的药物

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