Water solubilization capacity of pharmaceutical microemulsions based on Peceol®, lecithin and ethanol

• Ethanol induces fluidifying and disordering effect on the Peceol® supramolecular structure.
• Combination of ethanol and lecithin increases water solubilization of the Peceol®.
• The optimal ethanol/lecithin weight ratio in the Peceol® rich region is 40/60.
• Microemulsion properties are mainly influenced by ethanol partitioning.

Biocompatible microemulsions composed of Peceol®, lecithin, ethanol and water developed for encapsulation of hydrophilic drugs were investigated. The binary mixture Peceol®/ethanol was studied first. It was shown that the addition of ethanol to pure Peceol® has a significant fluidifying and disordering effect on the Peceol® supramolecular structure with an enhancement in water solubilization. The water solubilization capacity was improved by adding lecithin as a third component. It was then demonstrated that the ethanol/lecithin weight ratio played an important role in determining the optimal composition in term of water solubilization efficiency, a necessary property for a nutraceutical or pharmaceutical application. The optimal ethanol/lecithin weight ratio in the Peceol® rich region was found to be 40/60. Combination different techniques such as SAXS, fluorimetry, rheology and conductivity, we analyzed the water uptake within the microemulsion taking into account the partitioning of ethanol between polar and apolar domains. This ethanol distribution quantified along a water dilution line has a major effect on microemulsion properties.

Schematic representation of ethanol partitioning between polar and apolar domains in the W/O microemulsion.Figure optionsDownload high-quality image (260 K)Download as PowerPoint slide