Designing a high-payload liquid formulation for a lipophilic weak base using our deep eutectic solvent technology

The antimycotic compound ITZ is extremely poorly water-soluble, which is mainly driven by its high lipophilicity. The oral solution as developed by the originator contains hydroxypropyl-β-cyclodextrin (40%), propylene glycol and hydrochloric acid (pH 2) as solubilising excipients. In spite of the cocktail of solubilisation strategies employed in this product (cyclodextrin complexation, cosolvency and pH-adjustment), the total ITZ concentration is only 10 mg/ml. In general, developing a high-payload solubilised formulation is difficult, given ITZ's low solubility in excipients. Harnessing the potential of our our deep eutectic solvent platform, we have designed a formulation that has equivalent biopharmaceutical performance but 14-fold higher ITZ loading than the marketed oral solution. These findings illustrate the potential of our technology for the formulation of lipophilic, poorly soluble weak bases.


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