Oculis patent protected technology is the result of 20+ years of academic research by Dr. Thorsteinn Loftsson, Dr. Einar Stefansson and co-workers. The emphasis has been on the effect cyclodextrin has on transfer of drugs across biological membranes and the use of cyclodextrin for eye formulations. Cyclodextrins are cyclic oligosaccharides with hydrophilic outer surface but slightly lipophilic inner surface. Cyclodextrins form water soluble complexes with many lipophilic and poorly water-soluble drugs.
Oculis has thoroughly investigated how cyclodextrin facilitate the transport of drugs through biological membranes, i.e. in which case they are of use and when they are not. Oculis has also investigated how cyclodextrin improve the transport of drugs from the surface into the posterior part of the eye. Cyclodextrin are already used for variety of approved drugs and food products.
Oculis discovered how cyclodextrin complexes can form nano-particles in aqueous solution. Oculis has investigated the effects of cyclodextrin nano-particles on transfer of drugs, e.g. dexamethasone and dorzolamide, from the surface of the eye into both anterior and posterior part of the eye.
The next step was to use the nanoparticles to form microparticles with limited water solubility (see figure).
The image shows schematic formation of a single complex of drug and cyclodextrin which gradually forms water soluble nano-particle and finally a bigger micro-particle. This is a reversible formation