Background: Among all cancers, lung cancer has high mortality among patients in most of the countries
in the world. Targeted delivery of anticancer drugs can significantly reduce the side effects and dramatically improve
the effects of the treatment. Folate, a suitable ligand, can be modified to the surface of tumor-selective drug delivery
systems because it can selectively bind to the folate receptor, which is highly expressed on the surface of lung tumor
Objective: This study aimed to construct a kind of folate-targeted topotecan liposomes for investigating their efficacy
and mechanism of action in the treatment of lung cancer in preclinical models.
Methods: We conjugated topotecan liposomes with folate, and the liposomes were characterized by particle size,
entrapment efficiency, cytotoxicity to A549 cells and in vitro release profile. Technical evaluations were performed
on lung cancer A549 cells and xenografted A549 cancer cells in female nude mice, and the pharmacokinetics of the
drug were evaluated in female SD rats.
Results: The folate-targeted topotecan liposomes were proven to show effectiveness in targeting lung tumors. The
anti-tumor effects of these liposomes were demonstrated by the decreased tumor volume and improved therapeutic
efficacy. The folate-targeted topotecan liposomes also lengthened the topotecan blood circulation time.
Conclusion: The folate-targeted topotecan liposomes are effective drug delivery systems and can be easily modified
with folate, enabling the targeted liposomes to deliver topotecan to lung cancer cells and kill them, which could be
used as potential carriers for lung chemotherapy.