Effects of molecular characteristics of macromolecular drugs and selection of permeation enhancer on oral absorption
Improving our mechanistic knowledge of the influence of specific molecular descriptors of bRo5 drugs on oral absorption
Details
- Funder: Vinnova
Research scientist: Prosper Emeh, MSc.
Principal investigator: Professor Christel Bergström, Department of Pharmacy, Uppsala University.
Scientific and industrial context: The oral delivery of macromolecular drugs, beyond Lipinski’s Rule of 5 chemical space, such as peptides, proteins, and oligonucleotides, even when co-administered with transient permeation enhancers (TPEs), still presents the problem of a low (single digit) and variable bioavailability.
Aim: The project aims to study the physicochemical characteristics of beyond-the-rule-of-5 (bRo5) drugs and TPEs, explaining their interaction and the interplay with gastrointestinal barriers to improving oral bioavailability.
Outcome: We expect to improve our mechanistic knowledge of the influence of specific molecular descriptors of bRo5 drugs on oral absorption. The generated data could provide more insight into the macromolecule/permeation enhancer axis, possibly enabling a rational selection of TPEs while considering the physical-chemical properties of the orally administered macromolecule.