Smart Design of Targeted Drug Delivery System for Precise Drug Delivery and Visual Treatment of Brain Gliomas

Abstract In the treatment of glioma, which is one of the malignant tumors, although chemotherapy is used as the most common treatment method, it often suffers from low bioavailability. Therefore, improving the precision and efficiency of drugs is crucial in treating gliomas and a great challenge. Here, an advanced drug delivery system is reported for gliomas (CZQD@HA@DOX), which aggregates multiple features such as the susceptible imaging tracer property due to the use of CZQD and the targeting of HA to the receptor cluster 44 (CD44) of glioma cells, which provides the system with the functions of targeted enrichment and precise drug delivery at the tumor site. The pH‐responsive drug delivery system has not only an excellent encapsulation rate but also a high drug loading capacity, and the doxorubicin loaded on it can be released centrally at the tumor microenvironment site and causes an increase of reactive oxygen species in the mitochondria and trigger oxidative stress, which leads to high expression of Bax apoptotic proteins, ultimately activating the mitochondrial pathway‐mediated apoptotic process in glioma cells. Overall, this drug delivery system has great potential for application in precision targeted therapy and visual tracer imaging of gliomas.