The in vivo drug delivery pattern of the organelle-targeting small molecules

Eukaryotic cell organelles sustain the life of cells. Their structural changes and dysfunctions can cause abnormal physiological activities and lead to various diseases. Molecular imaging technology enables the visualization of subcellular structures, cells, organs, and the whole living body’s structure and metabolism dynamic changes. This could help to reveal the pharmacology mechanisms and drug delivery pathway in vivo. This article discusses the relationship between organelles and human disease, reviews recent probes targeting organelles and their behavior in vivo. We found that mitochondria-targeting probes prefer accumulation in the intestine, heart, and tumor. The lysosome-targeting probe accumulates in the intestine and tumor. Few studies on endoplasmic reticulum- or Golgi apparatus-targeting probes have been reported for in vivo imaging. We hope this review could provide new insights for developing and applying organelle-targeting probes.