Poor water solubility limits the absorption of many small molecule therapies. If an active ingredient cannot be solubilized in the gastric and intestinal media, it will not pass through the walls of the gastrointestinal tract and thus will be excreted from the body. This is a major barrier preventing new medicines from reaching the market.
Lipid-based formulations are well-known to enhance the absorption of water insoluble small molecules. The approach is simple: dissolve the drug in a lipid and administer the formulation. A drawback of this approach is that only the most lipophilic molecules have sufficient solubilities in the lipid vehicles. SeraNovo’s LiDES platform is perfectly suited to solve this problem.
Firstly, SeraNovo designs a eutectic composition of the active ingredient. This is a very high drug load mixture with e.g., 40% API. Secondly, a lipid vehicle is selected that can be used to dilute the eutectic composition. The result is a formulation with a high drug load with all the benefits that lipid-based formulations can offer, such as bioavailability enhancement or diminishing of food effects.
As an example, if a drug has a lipid solubility of 10 mg/mL and the required drug dose is 200 mg then 25 size 00 capsules would be required for a single treatment. With the LiDES platform the drug loading can be increased to such levels that only 1 capsule is required.
What drug molecules is the LiDES platform suitable for?
Perfect formulation approach for API’s that have:
Log P >4 Melting point <200°C