Júlio Ana, Costa João Guilherme, Pereira-Leite Catarina, Santos de Almeida Tânia
CBIOS-Universidade Lusófona's Research Center for Biosciences & Health Technologies, Campo Grande 376, 1749-024 Lisboa, Portugal.
Department of Biomedical Sciences, University of Alcalá, Ctra. Madrid-Barcelona Km. 33.600, Alcalá de Henares, 28871 Madrid, Spain.
Nanomaterials (Basel). 2021 Dec 21;12(1):7. doi: 10.3390/nano12010007.
Ionic liquids (ILs) have increasingly been studied as key materials to upgrade the performance of many pharmaceutical formulations. In controlled delivery systems, ILs have improved multiple physicochemical properties, showing the relevance of continuing to study their incorporation into these formulations. Transfersomes are biocompatible nanovesicular systems, quite useful in controlled delivery. They have promising characteristics, such as elasticity and deformability, making them suitable for cutaneous delivery. Nonetheless, their overall properties and performance may still be improved. Herein, new TransfersomILs systems to load rutin were developed and the physicochemical properties of the formulations were assessed. These systems were prepared based on an optimized formulation obtained from a Box-Behnken factorial design (BBD). The impact of imidazole-based ILs, cholinium-based ILs, and their combinations on the cell viability of HaCaT cells and on the solubility of rutin was initially assessed. The newly developed TransfersomILs containing rutin presented a smaller size and, in general, a higher association efficiency, loading capacity, and total amount of drug release compared to the formulation without IL. The ILs also promoted the colloidal stability of the vesicles, upgrading storage stability. Thus, ILs were a bridge to develop new TransfersomILs systems with an overall improved performance.
离子液体（ILs）作为提升多种药物制剂性能的关键材料，受到了越来越多的研究。在控释系统中，离子液体改善了多种物理化学性质，这表明继续研究将其纳入这些制剂具有重要意义。传递体是生物相容性纳米囊泡系统，在控释方面非常有用。它们具有诸如弹性和可变形性等有前景的特性，使其适用于经皮给药。然而，它们的整体性质和性能仍可能有待改进。在此，开发了用于负载芦丁的新型传递体 - 离子液体（TransfersomILs）系统，并评估了制剂的物理化学性质。这些系统是基于从Box - Behnken析因设计（BBD）获得的优化配方制备的。最初评估了基于咪唑的离子液体、基于胆碱的离子液体及其组合对HaCaT细胞活力和芦丁溶解度的影响。与不含离子液体的制剂相比，新开发的含芦丁的传递体 - 离子液体呈现出更小的尺寸，并且总体上具有更高的包封效率、载药量和药物释放总量。离子液体还促进了囊泡的胶体稳定性，提升了储存稳定性。因此，离子液体是开发具有整体性能改善的新型传递体 - 离子液体系统的桥梁。
