Arterial drug delivery requires optimizing injection and hemodynamic parameters and developing drugs and carriers with high tissue avidity. The complexity of the problem requires efficient high-volume research. The ideal tissue drug concentration measurements for arterial drug delivery should be site-specific, tissue-noninvasive, non-destructive, physiologically inert, repeatable, safe, cost-effective, and in a sub-second time domain while enabling concurrent blood flow assessment. They should be able to track drug concentration changes over time. Optical methods can significantly advance arterial pharmacokinetic research. This chapter introduces optical techniques from an arterial pharmacokinetic researcher’s perspective. It also makes the case for optical engineers to develop novel optical tools for arterial pharmacokinetic research.