BEPO^®: Injectable in-situ forming depots for the sustained release of active pharmaceutical ingredients

MedinCell is a French company that develops technologies for the sustained release of active pharmaceutical ingredients (API). The company mission to make medicine affordable to all is at the center of all research and development projects. Its core technology, BEPO^®, is based on bioresorbable amphiphilic block copolymers that once mixed with the API and a biocompatible solvent will yield injectable solutions or suspensions, depending on the solubility of the API. Upon injection into an aqueous medium, such as the subcutaneous (SC) environment, the copolymers will precipitate forming a depot which physically entraps the API. The subsequent release of therapeutic active molecules will be driven by their diffusion and copolymer degradation.

BEPO^® formulations utilize combinations of (m)PEG-b-PLA based di- and triblock copolymers for achieving the sustained release of API. The ratio between the hydrophobic and hydrophilic blocks, the length of each block, the triblock/diblock ratio, the copolymer content or the loading of API can be tuned to ensure plasmatic concentrations within the therapeutic window for a desired duration. The viscosity and the injectability of the formulations as well as the degradation kinetics of the depots are considered while formulating drug products and can be tailored depending on the foreseen application. Importantly, it has been demonstrated in animal models that, when administered SC, the depot can be located and monitored over time by ultrasounds echography. It is expected that, in case of emergency, it will be possible to easily locate the depot, which would enable its exeresis. MedinCell is also developing tools which mimic in-vivo SC conditions in order to enhance the predictability of in-vitro results during the formulation process.

BEPO^® is currently being used for producing best-in-class products for a wide range of drugs for different treatments including schizophrenia, depression, pain, contraception or anesthesia; two of these products are already undergoing clinical trials.