Local intestinal generation of transient permeability enhancers by digestion of lipid formulations (finished project)

Research scientist: Ann-Christin Jacobsen, PhD
Principal investigator: Associate Professor Alexandra Teleki, Department of Pharmacy, Uppsala University

Scientific and industrial context: Despite single digit bioavailability and high variability, permeation enhancer-based delivery systems for oral systemic delivery of macromolecules such as peptides and proteins have reached the clinics with two recent approvals (Mycapssa® and Rybelsus®).

Aim: To investigate if lipid-based formulations such as self-emulsifying drug delivery systems (SEDDS) that release permeation enhancing medium chain fatty acids upon digestion can improve the efficiency of permeation enhancer-based drug delivery systems. In vitro lipolysis will aid designing lipid-based formulations with defined permeation enhancer release. The formulations will be evaluated in in vitro and/or in vivo absorption and stability models.

Outcome: This project will reveal if intestinal digestion can be harnessed for increased permeation enhancer efficiency. Formulation design guided by lipolysis will generate information on medium chain lipid digestion kinetics and how macromolecular drugs in lipid-based formulations are affected by digestion.