Abstract

Many pharmaceutical compounds are poorly water soluble compounds showing poor and variable absorption in the gastro-intestinal tract. Lipid-based formulations provide a way to overcome poor oral bioavailability and food effects for certain of these challenging compounds. The developed lipid-based formulations can be administered orally by encapsulating the formulations in a softgel or hard capsule dosage form.

The presentation will discuss the characteristics of compounds which are appropriate candidates for a lipid-based formulation approach and will describe how appropriate excipients are selected based on the physico-chemical and biological characteristics of the compound. The design of lipid-based formulations using the selected excipients will be elucidated with a focus on self-(micro)emulsifying lipid-based formulation development.

To select the lipid-based formulations which will provide the optimal in vivo performance, in vitro dispersion and digestion testing are available as in vitro tools to predict in vivo behavior of the lipid-based formulations. These tools simulate the dispersion of a lipid-based formulation in the stomach as the formulation is released from the capsule dosage form, potentially followed by digestion of the dispersed lipid-based formulation in the small intestine. Both in vitro dispersion and digestion testing will be discussed in the presentation and its application will be demonstrated by a number of case studies. 

Last but not least, the presentation will describe the encapsulation of lipid-based formulations in a softgel or hard capsule dosage form to obtain suitable Drug Delivery Systems for oral delivery of lipid-based formulations capable of overcoming poor bioavailability and food effects of challenging compounds.