Radiotherapy is a well-established cytotoxic
therapy for local solid
cancers, utilizing high-energy ionizing radiation to destroy
cancer cells. However, this method has several limitations, including low radiation energy deposition, severe damage to surrounding normal cells, and high
tumor resistance to radiation. Among various
radiotherapy methods,
boron neutron capture therapy (BNCT) has emerged as a principal approach to improve the therapeutic ratio of
malignancies and reduce lethality to surrounding normal tissue, but it remains deficient in terms of insufficient
boron accumulation as well as short retention time, which limits the curative effect. Recently, a series of radiosensitizers that can selectively accumulate in specific organelles of
cancer cells have been developed to precisely target
radiotherapy, thereby reducing side effects of normal tissue damage, overcoming radioresistance, and improving radiosensitivity. In this review, we mainly focus on the field of nanomedicine-based
cancer radiotherapy and discuss the organelle-targeted radiosensitizers, specifically including nucleus, mitochondria, endoplasmic reticulum and lysosomes. Furthermore, the organelle-targeted
boron carriers used in BNCT are particularly presented. Through demonstrating recent developments in organelle-targeted radiosensitization, we hope to provide insight into the design of organelle-targeted radiosensitizers for clinical
cancer treatment.