Human Cytotoxicity, Hemolytic Activity, Anti-Inflammatory Activity and Aqueous Solubility of Ibuprofen-Based Ionic Liquids

Ionic liquids (ILs) are a potential solution to the general problem of low solubility, polymorphism and bioavailability active pharmaceutical ingredients (APIs). In this work, we report on synthesis three pharmaceutically ILs (API-ILs) based ibuprofen, one most commonly available over-the-counter nonsteroidal anti-inflammatory drugs (NSAIDs), with imidazolium cations ([C2C1Im][Ibu] [C2(OH)C1Im][Ibu]) cholinium cation ([N1112(OH)][Ibu]). An upgrade aqueous solubility (water biological simulated fluids) for ibuprofen-based relative ibuprofen’s neutral salt form (sodium ibuprofen) was verified. The cytotoxic profiles synthesized API-ILs were characterized using two human cells lines, Caco-2 colon carcinoma HepG-2 hepatocellular cells, up maximum plasma concentration (Cmax) without impairing their cytotoxicity response. Additionally, EC50 in cell line revealed similar results both parent APIs API-ILs. biocompatibility also evaluated through hemolytic activity assay, showed that all hemocompatible at concentrations higher than ibuprofen Cmax. Moreover, properties assessed inhibition bovine serum albumin (BSA) denaturation cyclooxygenases (COX-1 COX-2). [C2C1Im][Ibu], [C2(OH)C1Im][Ibu] [N1112(OH)][Ibu] maintained response improved selectivity towards COX-2, allowing development safer NSAIDs recognition new avenues selective COX-2 inhibitors cancer chemotherapy neurological diseases such as Alzheimer’s Parkinson’s.