Improvement of New Dianionic Ionic Liquids vs Monoanionic in Solubility of Poorly Water-Soluble Drugs

作者: José M.S.S. Esperança , Patrícia M. Reis , Ana R. Jesus , Alexandre Paiva , Ana R.C. Duarte

DOI: 10.1016/J.XPHS.2021.01.014

关键词: ChemistryLipophilicityIbuprofenSolubilityPhosphonateAqueous solutionBioavailabilityIonic liquidPiroxicamNuclear chemistry

摘要: Abstract New ionic liquids (ILs) based on dianionic phosphonate anions and ammonium cations were prepared characterized. They used as excipients to increase the water solubility of two oral drugs, piroxicam ibuprofen, that are slightly soluble in water. An increment 300-fold was achieved for ibuprofen when compared with pure water, only 0.25 mol% IL Interestingly, this less toxic liquid [N4 1 2OH 2OH]2 [C2H5PO3], which presents an IC50 120 mM (≈0.25 mol%). On other hand, showed 480-fold same liquid, percentage. In contrast, monoanionic liquids, effect not so pronounced, a 10-fold obtained, presence 0.3 mol% IL. The lipophilicity (logP) drugs decreased these ILs. Cytotoxicity profile ILs determined they did show significant impact towards healthy fibroblasts. cytotoxicity also determined, cellular viability almost change 1 mM drug.

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