Ensuring reproducible oral bioavailability for poorly water-soluble APIs remains one of the key challenges formulation scientists are faced with today. Our deep eutectic solvent technology provides new opportunities to address this solubility problem.
ROBUST SOLUBILITY ENHANCEMENT
Our formulations present the API to the gastrointestinal fluids in predissolved form, thereby avoiding slow dissolution from the crystalline form. The state of API supersaturation thus generated provides for a greatly enhanced driving force for absorption. To inhibit API precipitation after release from the formulation, we inlcude excipients like polymers and surfactants in the formulation. The tunable polarity of our deep eutectic solvents implies that we can readily include high concentrations of these excipients.
HIGH API LOADINGS
One of the key benefits of our technology resides in its ability to create high-payload formulations across all API chemistries, including the so-called "brick-dust" APIs whose solubility problem is driven by extremely high melting point. These APIs are difficult to formulate via traditional solubilisation (too low solvent capacity offered by cosolvents, surfactants, lipids or cyclodextrins), spray drying (too low solubility in organic solvents) or melt processing (too high melting point). Our platform creates new possibilities to prevent these molecules from falling from the development pipeline.
To design our deep eutectic systems, we select excipients from a library that comprises hundreds of GRAS substances. As we typically use three, four or five excipients to construct our formulations, rather than relying on the use of one single cosolvent or surfactant, we reduce potential excipient-related side effects as these are typically related to exceeding a critical threshold level of a single component.
EASE OF MANUFACTURE
Bulk production of our formulations is conducted in a single-pot, solvent-free process at mildly elevated temperature. This process requires minimal development effort and is readily scaled up. The liquid formulation obtained via this procedure can directly be filled in capsules, vials or any other container type. This simple manufacturing process constitutes a great advantage over other solubility-enhancing approaches such as nanosuspensions or amorphous solid dispersions, which not only require intricate unit operations to produce the primary formulation (wet milling, melt extrusion or spray drying), but also need a series of downstream processing steps (drying, blending, granulation or compression) to produce the final dosage form.