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Published on: October 31, 2019
A Green Innovative Approach for Solubility Enhancement of Poorly Water-Soluble Drugs Using Choline Chloride-Polyol
Liga Petersone1, Rihards Mahinovs1, Zoltán Márk Horváth1
1Leading Research Group, Faculty of Pharmacy, Rīga Stradiņš University, LV-1007 Riga, Latvia.
Choline chloride-based eutectic solvents significantly enhance the solubility of poorly water-soluble drugs like ibuprofen, naproxen, and apigenin. These green chemistry solvents show great potential for developing advanced pharmaceutical drug delivery systems.
Area of Science:
- Pharmaceutical Technology
- Green Chemistry
- Materials Science
Background:
- Eutectic solvents offer innovative pharmaceutical applications within green chemistry.
- A knowledge gap exists regarding the systematic study of eutectic solvent properties and uses in pharmaceuticals.
Purpose of the Study:
- To prepare and characterize choline chloride-polyol eutectic solvents.
- To evaluate their efficacy in enhancing the solubility of poorly water-soluble drugs.
- To investigate component interactions within the eutectic solvents.
Main Methods:
- Eutectic solvents were prepared from choline chloride and polyols (sorbitol, xylitol, mannitol, isomalt) at various molar ratios.
- Characterization involved DSC, FTIR, refractive index, Karl Fischer titration, and loss on drying.
- Solubility enhancement was assessed using the shake-flask method for ibuprofen, naproxen, and apigenin.
Main Results:
- Eutectic solvents were successfully prepared with low water content (<3%).
- Significant solubility increases were observed: ~152-fold for ibuprofen, ~144-fold for naproxen, and ~188-fold for apigenin.
- Interactions between eutectic solvent components were confirmed through physical characterization.
Conclusions:
- Choline chloride-polyol eutectic solvents demonstrate substantial potential as solubility enhancers.
- These solvents can facilitate the development of novel drug delivery systems for poorly soluble compounds.
- The findings support the application of eutectic solvents in green pharmaceutical technology.
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