Bioavailability Enhancement

:: Overview :: Poorly Soluble Drugs :: Poorly Permeable Drugs


Hydrophilic therapeutic agents geneally exhibit poor membrane transport properties and can present enormous challenges in drug delivery (primarily due to their charge, size and stability profiles). In the absence of appreciable oral absorption, such drugs must be delivered invasively in order to by-pass the lipophilic biological membrane barriers. In order to help overcome such issues, we have developed our MacroSOLV® lipid-based technology platforms, allowing for the non-invasive delivery for small polar organics and macromolecules. Through complexation of the drug with various GRAS approved lipidic based systems (formulation composition dependant on the drug properties), we are able to achieve optimal presentation of the complexed drug to the absorption site. This then promotes absorption of the drug across the epithelial cell membranes of the intestinal tract allowing for successful delivery of the therapeutic agent.

Advantages of using the MacroSOLV® approach include:

• Optically clear, water-free, single phase formulations of hydrophilic materials in oil/organic solvent
• Simple, mild, ready scale-up. No chemistry or solvents
• Employs GRAS-approved ingredients
• Compositional versatility (solute, solvent and amphiphile)
• Capable of high loadings
• Structural and chemical stability
• Improved thermal stability (including freeze-thawing)
• Variety of presentations, e.g. as bulk oil, o/w emulsions
• Wide range of potential applications