Trombino Sonia, Siciliano Carlo, Procopio Debora, Curcio Federica, Laganà Annarita S, Di Gioia Maria Luisa, Cassano Roberta
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.
Pharmaceutics. 2022 Jan 30;14(2):333. doi: 10.3390/pharmaceutics14020333.
Owing to a growing awareness toward environmental impact, the use of safer and eco-friendly solvents like deep eutectic solvents (DESs), has recently undergone important growth in the pharmaceutical field, with regard to their application as non-aqueous liquid administration vehicles, since they do not carry the same risks of toxicity and handling as traditional organic solvents. Major attention has been given to the development of advantageous transdermal drug delivery systems, because of their ease of use and better acceptability. Here, we report the use of two different DESs, based on choline chloride, used as hydrogen bond acceptor (HBA), and ascorbic acid or propylene glycol, used as hydrogen bond donors (HBDs), able to enhance the solubility and the topical delivery of dapsone, representing a class IV drug. The interactions between the DESs' components and the drug were studied by performing DSC, FT-IR, and NMR analysis of the eutectic systems and the pure drug, confirming the establishment of H-bonds between the drug and the DESs' components. Diffusion and permeability studies, carried out in a Franz cell, showed an increase in permeability, highlighting the great potential of DESs as dissolution and permeation enhancers in the development of novel and more effective drug delivery systems in topical administration.
由于对环境影响的认识不断提高，像深共熔溶剂（DESs）这样更安全且环保的溶剂，近期在制药领域的应用有了显著增长，尤其是作为非水性液体给药载体，因为它们不像传统有机溶剂那样具有相同的毒性和操作风险。由于其使用方便且接受度更高，优势透皮给药系统的开发受到了主要关注。在此，我们报告了两种基于氯化胆碱的不同DESs的使用情况，氯化胆碱用作氢键受体（HBA），抗坏血酸或丙二醇用作氢键供体（HBDs），它们能够提高氨苯砜（一种IV类药物）的溶解度和局部给药效果。通过对共熔体系和纯药物进行差示扫描量热法（DSC）、傅里叶变换红外光谱（FT-IR）和核磁共振（NMR）分析，研究了DESs成分与药物之间的相互作用，证实了药物与DESs成分之间形成了氢键。在Franz扩散池进行的扩散和渗透性研究表明渗透性有所提高，突出了DESs作为新型更有效局部给药药物递送系统开发中的溶解和渗透促进剂的巨大潜力。
