基于L-氨酸和2-Hydroxypropyl-β-Cyclodextrin的深度乳房溶剂用于药物载体和透增强
Jianhua Lv1, Pan Wu1,2, Yaru Fang1
1Jihua Laboratory, Jihua Institute of Biomedical Engineering and Technology, Foshan, 528000, People's Republic of China.
AAPS PharmSciTech
|September 12, 2023
概括
这项研究开发了使用L-氨酸和2-propyl-β-cyclodextrin进行透皮药物递送的新型深度浸泡溶剂 (DES). 这些DES增强了药物溶解性和皮肤透性,对药物输送系统显示出前景.
科学领域:
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
- 生物技术是生物技术.
背景情况:
- 深度浸泡溶剂 (DES) 正在成为药物输送系统的有前途的辅助剂.
- 开发具有可调节性质的新型DES配方对于优化药物溶解性和通过皮肤透至关重要.
- 选择了L-氨酸和2-propyl-β-cyclodextrin (2HPβCD) 分别作为键受体 (HBA) 和供体 (HBD),以创建新的DESs.
研究的目的:
- 合成和描述由L-氨酸和2HPβCD组成的新型DES,含水量不同.
- 评估这些DES的物理化学性质,包括粘度,玻璃过渡温度和药物溶解度.
- 调查这些DES作为模范药物的通过皮肤递送药物系统 (TDDS) 的有效性.
主要方法:
- 使用L-氨酸 (HBA) 和2HPβCD (HBD) 制备DES,其质量比为4:1,含水量为40-60%.
- 减弱总反射里埃变换红外线 (ATR-FTIR) 和1H核磁共振 (1H-NMR) 光谱法用于确认DES合成.
- 评价了粘度,玻璃过渡温度 (Tg),模型药物的溶解度 (易布洛芬,诺弗洛克萨,纳特格林尼德) 和在体外通过皮肤吸收利多卡因.
主要成果:
- 通过光谱分析证实了DESs的成功合成.
- 增加的水含量 (45-60%) 降低了DES粘度,增加了Tg.
- 与水相比,在DES中药物溶解性显著提高,并且证明了利多卡因的透,其中包括脂质流化和质结构改变的机制.
结论:
- 开发的基于L-氨酸/2HPβCD的DES对TDDS具有有利的物理化学特性.
- 这些DES显示出出色的药物溶解和通过皮肤透的增强能力.
- 可调节的性质和非刺激性质表明在药物溶解和通过皮肤递送中具有广泛的适用性.
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