Despite being one of the most effective broad-spectrum chemotherapeutic agents in the treatment of cancers,
the clinical applications of bleomycins (BLMs) have been limited due to their poor drug delivery abilities, and the side effect
of causing lung fibrosis. With the increased therapeutics and the reduction of side effects, research and development of
targeted drug delivery systems (TDDS) with BLMs have become essential for the expansive clinical usage of BLM-based
therapeutics. This review summarizes the recent developments of various TDDS for BLMs, including techniques such as
photochemical internalization, ultrasound, and micelle, liposome, and nanoparticle formation. The advantages and disadvantages
for each delivery approach are outlined, along with the specific challenges associated with each delivery system.