Jorge Ludmilla R, Harada Liliam K, Silva Erica C, Campos Welida F, Moreli Fernanda C, Shimamoto Gustavo, Pereira Jorge F B, Oliveira José M, Tubino Matthieu, Vila Marta M D C, Balcão Victor M
PhageLab - Laboratory of Biofilms and Bacteriophages of University of Sorocaba, Sorocaba, Brazil.
Institute of Chemistry, University of Campinas, Campinas, Brazil.
Front Pharmacol. 2020 Apr 23;11:243. doi: 10.3389/fphar.2020.00243. eCollection 2020.
In this research project, synthesis and characterization of ionic liquids and their subsequent utilization as facilitators of transdermal delivery of human insulin was pursued. Choline geranate and choline oleate ionic liquids (and their deep eutectic solvents) were produced and characterized by nuclear magnetic resonance (H NMR), water content, oxidative stability, cytotoxicity and genotoxicity assays, and ability to promote transdermal protein permeation. The results gathered clearly suggest that all ionic liquids were able to promote/facilitate transdermal permeation of insulin, although to various extents. In particular, choline geranate 1:2 combined with its virtually nil cyto- and geno-toxicity was chosen to be incorporated in a biopolymeric formulation making it a suitable facilitator aiming at transdermal delivery of insulin.
在本研究项目中,开展了离子液体的合成与表征,并随后将其用作人胰岛素经皮递送的促进剂。制备了胆碱香叶酸酯和胆碱油酸酯离子液体(及其低共熔溶剂),并通过核磁共振(H NMR)、水分含量、氧化稳定性、细胞毒性和遗传毒性测定以及促进经皮蛋白质渗透的能力对其进行了表征。收集到的结果清楚地表明,所有离子液体都能够促进/协助胰岛素的经皮渗透,尽管程度不同。特别是,胆碱香叶酸酯1:2结合其几乎为零的细胞毒性和遗传毒性,被选择纳入生物聚合物配方中,使其成为用于胰岛素经皮递送的合适促进剂。