A Self-Emulsifying Drug Delivery System (SEDDS) approach was taken by Pii to improve the bioavailability and solubility of a hydrophobic compound. The customer previously had been evaluating an IV formulation, but wanted to consider an oral drug product for patient convenience and compliance. The compound was a BCS-IV drug, no water solubility, very poor lipid solubility, and low permeability. Various approaches had been previously screened, including cyclodextrins and combinations of surfactants and solubility enhancers. Pii’s formulation team was able to develop a soft gel formulation that facilitated good oral dissolution, and as well as improved absorption to the intended site. This involved the combination of oil and polymers, which included surfactant/co-surfactant and emulsifier.

Stable formulations using Pii’s approach provided a greater than ten-fold increase in drug solubility. And, a bioavailability study comparing the suspension lipidic vehicle in a soft gel dosage form versus neat API resulted in an increase of more than 100-fold in bioavailability.