Enhanced in vitro cytotoxicity and intracellular uptake of Genipin via loaded on Nano-Liposomes made from soy lecithin in MCF-7 cells

Document Type : Research Paper


1 Nano Drug Delivery Research Center, Health Technology Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran

2 Substance Abuse Prevention Research Center, Health Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran

3 Pharmaceutical Research Center, Health Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran


Objective(s): As an alternative to chemical drugs, natural compounds such as Genipin can reduce toxicity and side effects. In recent years, Genipin's antioxidant properties have been considered a potential cancer treatment. Therefore, the present study investigated anti-cancer activity of newly formulated nano-liposomal loaded Genipin, made from soy lecithin, against MCF-7 cancer cell line.

Materials and Methods: After synthesis, the physicochemical properties of the liposomes were confirmed by Dynamic light scattering (DLS), Scanning Electron Microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), and UV-vis spectrophotometry.

Results: Our results showed that the prepared nano-liposome had a diameter of 166.2 nm. Its Zeta potential was -25.4 mV which indicates the good electrostatic stability of nano-liposomes. Also, a slight size distribution (PDI 0.2870) and a high encapsulation efficiency (EE% >82% and DL>28%) are other features of synthesized nano-liposomal loaded Genipin. The in vitro result profile demonstrated that the drug-controlled release from Genipin loaded-liposomal is 65% during 70h. The in vitro cytotoxic activity of nano-liposomal loaded Genipin in comparison with free Genipin, was explored on MCF-7 cell line using MTT colorimetric assay. Our results revealed that the IC50% (cytotoxicity) of MCF-7 cells treated with nano-liposomes loaded Genipin were higher than those treated with free Genipin (about 2.4 orders of magnitude). Additionally, cell uptake studies evidenced a higher uptake of negative nano-liposomal loaded Genipin.

Conclusion: In a nutshell, newly formulated nano-liposomal is an ideal vehicle for negative targeting (anticancer effect) of drugs to tumor cells that may result in improved efficacy and reduced toxicity of encapsulated drug moiety.