Photoacoustic imaging (PAI) is rapidly becoming established as a viable imaging modality for small animal research, with promise of near-future human clinical translation. In this review, we discuss emerging prospects for photoacoustic-guided drug delivery. PAI presents opportunities for applications related to drug delivery, mainly with respect to either monitoring drug effects or monitoring drugs themselves. PAI is well-suited for imaging disease pathology and treatment response. Alternatively, PAI can be used to directly monitor the accumulation of various light-absorbing contrast agents or carriers with theranostic properties.