Preparation and evaluation of gemcitabin and cisplatin-entrapped Folate-PEGylated liposomes as targeting co-drug delivery system in cancer therapy

Abstract

In this research, we reported the preparation and properties of lipid-loaded nanoparticle modified with polyethylene glycol (PEG) and folic acid (FA) as a co-drug delivery system for controlling the release of cisplatin (Cis) and gemcitabine (Gem). Then, LIP-PEG-FA-Cis-Gem nano-complex was characterized by FT-IR, DLS, TEM, SEM, and XRD. The results suggest that these nano-complexes have spherical morphology with appropriate size and surface charge. The drug entrapment efficiencies were calculated about 22.96% (Cis) and 25% (Gem). In vitro drug release profile and then the therapeutic efficiency of LIP-PEG-FA-Cis-Gem nano-complex was also investigated on A549, MCF-7 and normal MRC5 cell lines. The cell viability value was observed 10.39 ± 4.88% (A549), 7.56 ± 4.87% (MCF7), and 23.2 ± 6.29% (MRC5) after 48 h of treatment with 8 μM concentration. Additionally, apoptosis amounts have indicated 83.0 ± 0.70% and 82.5 ± 0.21% for A549 and MCF7 cell lines after 48 h posttreatment, respectively. Moreover, the apoptotic P21 and P53 gene expression were observed 13.85 ± 0.73 and 17.16 ± 2.12 folds for A549, 6.78 ± 0.84 and 13.08 ± 0.84 folds for MCF7 after 48 h of incubation with LIP-PEG-FA-Cis-Gem IC50 concentrations, respectively. Therefore, our synthetic nano-liposome can be an excellent candidate for co-delivery of Gem & Cis agents to folat receptor-expressing tumors and the inhibition of cancer cells.