The introduction of a new drug entity to the clinic may take many years with a significant investment. Thus, only a few dozen of new drug entities are approved by the FDA each year. Chemical modification of existing drugs for improved properties or generating new IP, is considered a new drug entity and may require to pass a long and expensive approval process.
Our approach for improving drugs that are in clinical use, without chemical modification, is by finding them a new indication that they may be effective in, reformulating them into more effective and safe formulations or preparing reversible salts of the drug molecules.
The cannabinoids, CBD and THC, are water insoluble phenolic molecules with poor oral bioavailability. Oral formulation based on the pro-nano-liposphere (PNL) concept have been prepared and showed significant increase in oral bioavailability. The formulation consists of a solid lipid, surfactants and an edible solvent that the drug is soluble in, where upon addition to gastric fluid, it spontaneously forms nanoparticles that are capable to penetrate the gastrointestinal walls and reach the blood stream. Buccal formulation that provides CBD constant blood levels for over 8 hours, after a single application was demonstrated. CBD phenolate salts were prepared for improved stability and physical properties. Injectable formulations that release an active agent for several weeks, after a single injection have been developed. These concepts can be applied to many water insoluble drugs as well as phenol containing agents for improved drug activity.