: In the past decade, the glycol chitosan nanocarriers (GCNCs) have been widely used for tumor-targeted delivery of anticancer agents such as chemo drugs, peptides, and genes due to their biocompatibility, biodegradability, and easy fabrication. In particular, GCNCs can effectively solubilize water-insoluble chemo drugs as well as improve the delivery efficiency of chemo drugs to the tumor, resulting in maximizing therapeutic efficacy and minimizing side effect. In this review, we introduce the various applications of GCNCs for cancer treatment and these GCNCs demonstrate the great potential in overcoming challenges of chemotherapeutics. : Various designs of GC nanocarriers have been reviewed. The current state of GC nanocarriers for delivering chemotherapeutics with a focus on their physicochemical properties including solubilization of anti-cancer drugs, sustained release, and tumor-selectivity. Furthermore, state of the art in delivery and therapeutic strategy using GC nanocarriers also introduced for overcoming challenges of chemotherapeutics. : Based on the reviewed literature, physicochemical properties of GC nanocarriers will have a great potential to overcome challenges posed by chemotherapeutics.