Interactions of anticancer drugs with biomembranes: what can we learn from model membranes?

ABSTRACT

The interactions of anticancer drugs with cell membranes are of primary importance for drug transport, accumulation and activity. However, these interactions are very difficult to investigate because of the complexity of biological membranes. Lipid model membranes have therefore been built to gain insight into the collective role of lipids in drug-membrane interactions. Membranes can act as a barrier for drug molecules, sequester them or conversely may allow them to freely diffuse, thereby modulating the accumulation of drugs into cells. Lipid membranes also affect the ability of the efflux pump Pgp to bind and efflux anticancer drugs from cells. On the other hand, anticancer drugs can alter the structure and properties of lipid membranes, which are expected to influence the functioning of embedded proteins. The relevance of lipid model membranes to assess interactions between anticancer drugs and biomembranes is evidenced.