Enhancement of water solubility of poorly water-soluble drugs by new biocompatible N-acetyl amino acid N-alkyl cholinium-based ionic liquids
| Autor: | Patrícia M. Reis, Luís Raposo, José M. S. S. Esperança, Mário R. C. Soromenho, Alexandra R. Fernandes, Ana R. Jesus, Pedro V. Baptista |
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| Rok vydání: | 2019 |
| Předmět: |
Diclofenac
Cell Survival Chemistry Pharmaceutical Ionic Liquids Pharmaceutical Science 02 engineering and technology 030226 pharmacology & pharmacy Choline 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Humans Organic chemistry Amino Acids Cells Cultured Alkyl Acetaminophen chemistry.chemical_classification Aqueous solution Chemistry Water General Medicine Diclofenac Sodium Fibroblasts 021001 nanoscience & nanotechnology Bioavailability Partition coefficient Solubility Drug delivery Lipophilicity Ionic liquid Solvents 0210 nano-technology Hydrophobic and Hydrophilic Interactions Biotechnology |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 137:227-232 |
| ISSN: | 0939-6411 |
| Popis: | The major challenge of the pharmaceutical industry is to find potential solvents for poorly water-soluble drug molecules. Ionic liquids (ILs) have attracted this industry as (co-) solvents due to their unique physicochemical and biological properties. Herein, a straightforward approach for the enhancement of the water solubility of paracetamol and sodium diclofenac is presented, using new biocompatible N-acetyl amino acid N-alkyl cholinium-based ionic liquids as co-solvents (0.2–1 mol%). These new ionic liquids were able to increase the water solubility of these drugs up to four times that in pure water or in an inorganic salt solution. In the presence of these ILs, the drugs lipophilicity (log P was not significantly changed for paracetamol, but for sodium diclofenac it was possible to decrease significantly its lipophilicity. Concerning cytotoxicity in human dermal fibroblasts it was observed that ILs did not show a significant toxicity, and were able to improve cell viability compared with the respective precursors. |
| Databáze: | OpenAIRE |
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