The Impact of Water on Choline‐2‐Octenoic Ionic Liquid‐Facilitated Transdermal Transport
The Impact of Water on Choline‐2‐Octenoic Ionic Liquid‐Facilitated Transdermal Transport
复制标题
水对胆碱的影响—2—辛烯离子液体—促进透皮运输
DOI：
10.1002/adtp.202200096
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发表时间：
2022
影响因子：
4.6
通讯作者：
Kundu, Santanu
中科院分区：
文献类型：
--
作者：
Nichols, Isabel R.;Hamadani, Christine M.;Chism, Claylee M.;Hunter, Alysha N.;Ahmad, Humayun;Wontor, Kendall;Williams, Ashley E.;Vashisth, Priyavrat;Hammer, Nathan I.;Kundu, Santanu
离子液体 (IL) 已被证明是药物活性成分（包括小分子和蛋白质）的有效透皮渗透剂。离子液体中水的存在已被证明在其分子水平的结构组织中发挥着关键作用。然而，水对 IL 透皮转运功效的影响仍有待研究。在此，测试了水浓度梯度 (0%–100% v/v)，以评估离体猪皮肤模型中胆碱反式 2-辛烯酸 (CA2OE) 介导的亲水性模型药物葡聚糖 (10000 Da) 的转运。与 2:1、1:1、1:4 和 1:5 离子比制剂相比，50% v/v CA2OE 1:2-水证明在将葡聚糖转运至受体液体方面取得了最大的成功。进行物理化学表征（动态光散射 (DLS)、扫描电子显微镜 (SEM)、光密度 (O.D.)、傅里叶变换红外光谱 (FTIR)、荧光显微镜和流变学）来测试本体和纳米级 CA2OE 1:2-水相互作用。据推测，与 50% 相比，CA2OE 1:2 75% v/v 制剂中微乳液的存在导致转运严重下降。因此，在配制用于透皮运输应用的白细胞介素时，全面考虑白细胞介素成分、共溶剂和药物分子之间的相互作用至关重要。
Ionic liquids (ILs) have been shown to be effective transdermal penetrants of pharmaceutically active ingredients, including small molecules and proteins. The presence of water within ionic liquids has been demonstrated to play a critical role in their structural organization on the molecular level. However, the impact of water on IL transdermal transport efficacy has yet to be investigated. Herein, a water concentration gradient (0%–100% v/v) is tested to evaluate choline trans‐2‐octenoic (CA2OE)‐mediated transport of a hydrophilic model drug dextran (10000 Da) in an ex vivo porcine skin model.Compared to 2:1, 1:1, 1:4, and 1:5 ionic ratio formulations, 50% v/v CA2OE 1:2‐water evidences the greatest success at transporting dextran to the acceptor fluid. Physicochemical characterization (dynamic light scattering (DLS), scanning electron microscopy (SEM), optical density (O.D.), Fourier transform infrared spectroscopy (FTIR), fluorescent microscopy, and rheology) is conducted to test both bulk and nanoscale‐level CA2OE 1:2–water interactions. It is hypothesized that the presence of microemulsions in the CA2OE 1:2 75% v/v formulation accounted for the severely decreased transport compared to the 50%. It is thus critical to comprehensively consider interactions between IL components, co‐solvents, anddrug molecules when formulating ILs for transdermal transport applications.