Solubility improvement of atorvastatin using deep eutectic solvents.

Area of Science:

• Pharmaceutical Science
• Materials Science

Background:

• Deep eutectic solvents (DESs) offer potential in pharmaceuticals but require safety and usability assessments.
• Improving drug solubility is crucial for effective drug delivery and formulation.

Purpose of the Study:

• To investigate the potential of DESs to enhance the solubility of atorvastatin calcium trihydrate (ATCH).
• To explore eutectic interactions between ATCH and coformers like nicotinamide (NA) within a DES system.

Main Methods:

• Utilized co-crystallization principles to form eutectic mixtures.
• Employed polarization microscopy, Fourier transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC) for analysis.
• Evaluated interactions between ATCH, nicotinamide (NA), and propylene glycol (PG) in a DES.

Main Results:

• Identified an optimal DES system using nicotinamide (NA) in propylene glycol (PG) for ATCH.
• Confirmed hydrogen bond (H-bond) formation between ATCH and DES components via FT-IR and DSC.
• Demonstrated a significant increase in ATCH solubility in the DES system (0.158 ± 0.098 mg/mL) compared to water (0.000597 ± 0.003 mg/mL).

Conclusions:

• Deep eutectic solvents, particularly with nicotinamide as a coformer in propylene glycol, effectively enhance atorvastatin calcium trihydrate solubility.
• The study validates the use of DESs as a viable strategy for improving the solubility of poorly soluble drugs like ATCH.
• Hydrogen bonding interactions are key to the enhanced solubility observed in the DES system.