Folate-modified, cisplatin-loaded lipid carriers for cervical cancer chemotherapy

Background: Cervical cancer chemotherapy calls for the efficiently delivery of anticancer drug into cancer cells by nanoparticles. In this study, folate (FA) modified, cisplatin (CIS)-loaded nanostructured lipid carriers (NLCs) were constructed and evaluated. Methods: FA containing polyethylene glycol (PEG)-distearoylphosphatidylethanolamine (DSPE) (FA-PEG-DSPE) was synthesized. FA-PEG-DSPE modified, CIS-loaded NLCs (FA-CIS-NLCs) were prepared. Their particle size, zeta potential, drug encapsulation efficiency (EE) and in vitro delivery behavior were evaluated. In vitro cytotoxicity study of FA-CIS-NLCs was tested in human cervix adenocarcinoma cell line (HeLa cells). In vivo anti-tumor efficacies of the carriers were evaluated on a mice-bearing cervical cancer model. Results: The optimum FA-CIS-NLCs formulations have a particle size of 143.2 nm and a +25.7 mV surface charge. FA-CIS-NLCs displayed the best anti-tumor activity than other formulations in vitro and in vivo. Conclusions: The results demonstrated that FA-CIS-NLCs were efficient in selective delivery to cancer cells over-expressing FA receptors (FRs). FA-CIS-NLCs targeted transfer CIS to the cervical cancer cells, enhance the anti-tumor capacity. The novel constructed NLCs could function as outstanding nanocarriers for the delivery of drugs for the targeted treatment of cervical cancers.