Solid Lipid Solutions as Formulation Platform for Poorly Soluble Drugs

16:15 - 16:50

Vast majority of new active pharmaceutical ingredients (APIs) entering development pipeline from discovery possess insufficient water solubility and/or low dissolution rate. These cause challenges in achieving desired bioavailability.

Formulating API as a lipid-based formulation is often taken as approach to achieve desired bioavailability. This is achieved mainly by enhancements in drug solubilization and dissolution rate. In addition, LBF can stimulate intestinal lymphatic drug transport (thereby reducing first-pass metabolism), and merging evidence suggests a potential role for components of LBF (primarily surfactants) in the inhibition of intestinal efflux and metabolism. Most common way to formulate the LBFs is soft capsule approach where API is dissolved or suspended in liquid vehicle. However, using a semi-solid or solid carrier to form solid lipid solution (SLS) can offer many advantages such as possibility for manual filling at small scale in lab environment for purpose of pre-clinical and early clinical studies. Selection of excipients for SLS is made based on automated solubility screening of API in solid lipid excipients. Combination of these two techniques significantly reducing time and cost for development and manufacturing of pre-clinical and early clinical formulation of ‘difficult-to-formulate’ compounds.

Ruzica Kolakovic, Senior Scientist, Pharmaceutical Sciences, Drug Product Development , Janssen