Abstract
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 (1H 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.
Highlights
Insulin therapy is used in the treatment of Diabetes Mellitus, controlling hyperglycemia in patients suffering from type-1 diabetes
When insulin production is deficient, glucose accumulates in the blood and urine, leading to the destruction of cells due to a lack of supply and consequent onset of the condition known as Diabetes mellitus
In the research effort just described, synthesis of ionic liquids (ILs) and their DES was pursued aiming at their use as potential enhancers of insulin transdermal permeation, followed by their physicochemical and biological characterization
Summary
Insulin therapy is used in the treatment of Diabetes Mellitus, controlling hyperglycemia in patients suffering from type-1 diabetes. A major drawback of the current forms of insulin therapy lies in their invasive nature This has prompted the development of an artificial pancreas with a closed-loop system, and exploration of newer insulin delivery methods such as transdermal, buccal, oral, pulmonary, nasal, ocular and rectal routes (Mamatha et al, 2015). In order to overcome this obstacle, and to allow insulin absorption, various methods of weakening the stratum corneum have been tested over time, namely methods including absorption promoters, iontophoresis, sonophoresis, and micro-needles (Lassmann-Vague and Raccah, 2006; Khafagy et al, 2007). Variation in human skin permeability has been reported even among individuals (both inter- and intra-individual variations), and pig skin is frequently used as an alternative to human skin in percutaneous absorption studies aiming at developing transdermal formulations (Todo, 2017)
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