Abstract
Drug targeting is one of the promising approaches to increase the pharmacological activity of various kinds of therapeutic agents with a concomitant decrease in their unexpected side effects. To optimize the pharmacokinetic property of drug targeting vectors, pharmacokinetic analaysis should be important. Physiologically-based pharmacokinetic (PBPK) model has widely been established for various types of small molecules although such model analysis on macromolecules is still limited. PBPK model analysis can quantitatively describe the disposition of therapeutic agents. Several indices have been defined to characterize the drug targeting efficiency, and the feature of each index can be understood based on PBPK model. Sensitivity analysis based on PBPK model can reveal the most important factors affecting their pharmacological and/or toxicological effects. The other advantage of the PBPK model analysis includes the quantitative prediction of the biodistribution in humans based on the in vitro data. This review will summarize the importance of pharmacokinetic analaysis in the various aspects regarding the design of drug targeting vectors. Several examples for such approach will also be introduced and discussed.
