Choline geranate deep eutectic solvent/ionic liquid (CAGE) has shown several desirable therapeutic properties including antimicrobial activity and ability to deliver drugs transdermally in research laboratories. Here, we describe the first report of clinical translation of CAGE from the lab into the clinic for the treatment of rosacea, a common chronic inflammatory skin disorder that affects the face. We describe the seven steps of clinical translation including (a) scale‐up, (b) characterization, (c) stability analysis, (d) mechanism of action, (e) dose determination, (f) GLP toxicity study, and (g) human clinical study. We describe the challenges and outcomes in these steps, especially those that uniquely arise from the deep eutectic nature of CAGE. Our translational efforts led to a 12‐week open‐label phase 1b cosmetic study with CAGE_1:2 gel (CGB400) in mild–moderate facial rosacea in 26 patients where CGB400 exhibited a marked reduction in the number of inflammatory lesions. These results demonstrate the therapeutic potential of CGB400 for treating rosacea as well as it provides insights into the translational journey of deep eutectic solvents, in particular CAGE, for dermatological applications.

中文翻译：

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胆碱香叶酸低共熔溶剂的临床转化


香叶酸胆碱低共熔溶剂/离子液体 (CAGE) 已显示出多种理想的治疗特性，包括抗菌活性和在研究实验室中透皮输送药物的能力。在这里，我们描述了 CAGE 从实验室到临床用于治疗红斑痤疮的临床转化的第一份报告，红斑痤疮是一种影响面部的常见慢性炎症性皮肤病。我们描述了临床转化的七个步骤，包括 (a) 放大、(b) 表征、(c) 稳定性分析、(d) 作用机制、(e) 剂量确定、(f) GLP 毒性研究和 (g) ）人体临床研究。我们描述了这些步骤中的挑战和结果，特别是那些因 CAGE 的深层共晶性质而独特产生的挑战和结果。我们的转化工作导致了一项为期 12 周的开放标签 1b 期美容研究，使用 CAGE _1:2凝胶 (CGB400) 治疗 26 名患者的轻度至中度面部红斑痤疮，其中 CGB400 表现出炎症病变数量显着减少。这些结果证明了 CGB400 治疗红斑痤疮的治疗潜力，并为深入了解低共熔溶剂（特别是 CAGE）在皮肤病学应用中的转化历程提供了见解。