With a growing number of BCS-III and BCS-IV small molecules being developed, enabling oral dosage forms with acceptable oral bioavailability has become increasingly difficult and expensive, leading drug makers to resort to developing injectables. Many of these small molecules fall outside of “Lipinkski’s rule of 5”, leading to poor solubility and permeability characteristics.
Enteris uses its ProPerma® platform to improve both solubility and permeability of small molecules. The ProPerma® approach utilizes an enteric coating surrounding a tablet core containing the API with solubilizing agents that are also known to have permeation-enhancing properties. By delivering the formulation directly to the absorptive area of the small intestine, such permeability enhancers enable the transport of small molecules through the epithelium via passive movement across the tight junctions, or by the transcellular route, crossing the cell membrane.
Enteris has demonstrated positive results in enhancing the oral bioavailability of BCS-III and BCS-IV small molecules, in some cases providing more than 20-fold improvement in oral bioavailability. Enteris BioPharma is uniquely qualified to provide total integrated product development and enable the delivery of the most challenging small molecules.
