The biodistribution and pharmacokinetics of drugs are vital to the mechanistic understanding of their efficacy. Measuring antimicrobial drug efficacy has been challenging as plasma drug concentration is used as a surrogate for tissue drug concentration, yet typically does not reflect that at the intended site(s) of action. Utilizing an image-guided approach, it is feasible to accurately quantify the biodistribution and pharmacokinetics within the desired site(s) of action. We outline imaging modalities used in visualizing drug distribution with examples ranging from in vitro cellular drug uptake to clinical treatment of microbial infections. The imaging modalities of interest are: radio-labeling, magnetic resonance, mass spectrometry imaging, computed tomography, fluorescence, and Raman spectroscopy. We outline the progress, limitations, and future outlook for each methodology. Further advances in these optical approaches would benefit patients and researchers alike, as non-invasive imaging could yield more profound insights with a lower clinical burden than invasive measurement approaches used today.

药物的生物分布和药代动力学对于从机理上理解其功效至关重要。由于血浆药物浓度被用作组织药物浓度的替代指标，因此测量抗菌药物疗效一直具有挑战性，但通常不能反映预期作用部位的情况。利用图像引导的方法，准确量化所需作用部位内的生物分布和药代动力学是可行的。我们概述了用于可视化药物分布的成像方式，示例包括体外细胞药物摄取用于微生物感染的临床治疗。感兴趣的成像方式是：放射性标记、磁共振、质谱成像、计算机断层扫描、荧光和拉曼光谱。我们概述了每种方法的进展、局限性和未来前景。这些光学方法的进一步发展将使患者和研究人员受益，因为与当今使用的侵入性测量方法相比，非侵入性成像可以产生更深刻的见解，并且临床负担更低。