API-ILs Ionic Adducts: Solubility and Surface Activity Properties-En Route to New Paradigm in Drug Development

Area of Science:

• Pharmaceutical Chemistry
• Materials Science

Background:

• Hydrophobic active pharmaceutical ingredients (APIs) often exhibit poor solubility, limiting their formulation options.
• Guanidine derivatives are known for their high proton affinity, enabling strong interactions.

Purpose of the Study:

• To synthesize novel perfluoroalkyl ionic liquids with bicyclic guanidinium cations.
• To investigate their application as surfactant components for improving the solubility of hydrophobic APIs.
• To characterize the resulting API-IL ionic adducts.

Main Methods:

• Synthesis of two distinct perfluoroalkyl ionic liquids.
• Formulation of hydrophobic APIs with the synthesized ionic liquids.
• Solubility assessment of the resulting adducts, particularly for ophthalmic applications.

Main Results:

• The synthesized perfluoroalkyl ionic liquids significantly improved the solubility of selected hydrophobic APIs.
• Stable ionic adducts were formed between the ionic liquids and APIs containing carboxylic groups via hydrogen bonding.
• The enhanced solubility of the adducts is suitable for ophthalmic preparations, such as eye drops and lens care solutions.

Conclusions:

• Novel API-IL ionic adducts represent a new class of active derivatives with significant pharmaceutical potential.
• The unique properties of perfluoroalkyl ionic liquids facilitate the development of soluble drug formulations.
• These findings open avenues for advanced drug delivery systems, especially for ophthalmic applications.