The influence of serum lipoproteins on the pharmacokinetics and pharmacodynamics of lipophilic drugs and drug carriers.

One of the most ambitious goals in the therapy of human diseases is developing targeted drug delivery which would allow an effective concentration of drug to reach diseased sites while sparing non-diseased tissues. One of the most extensively researched approaches in controlled drug delivery has been the incorporation of drugs into lipid carriers or phospholipid vesicles, known as liposomes. However, the behavior of lipophilic drugs and liposomes within the circulating blood remains unknown. Several laboratories have demonstrated that the pharmacokinetics, tissue distribution, and pharmacological activity of a number of drugs incorporated into liposomes are influenced by their interaction with serum lipoproteins. This chapter will examine the influence of serum lipoproteins on the pharmacokinetics and pharmacodynamics of lipophilic drugs and drug carriers.