Preparation, properties and anti-tumor effect of the self-assemblies of a phosphoryl N-tetradecanoyl gemcitabine derivative / 国际药学研究杂志

ABSTRACT

Objective: To prepare the self-assemblies of a phosphoryl N-tetradecanoyl gemcitabine (CPTG) derivative and evaluate the properties and anti-tumor effect. Methods: CPTG derivative was synthesized. The prodrug membrane was investigated using a Langmuir trough. The self-assembly was prepared using the injection method. The morphology of self-assemblies was observed by a transmission electron microscope. The particle distribution was measured by a dynamic light scattering instrument. The pharmacodynamic effect was evaluated on HepG2 cells and tumor-bearing mice. Results: The prodrug was synthesized with gemcitabine as the raw material. The surface pressure-molecular area (π-a) curves at the air/water interface indicated that the prodrug was amphiphilic and formed the stable monolayer. The self-assemblies formed the vesicles with the mean size of 93.52 nm and the Zeta potential of -31 mV. The inhibitory effects of self-assemblies were significantly higher than those of gemcitabine on the models of HepG2 cells and the tumor-bearing mice. Conclusion: The self-assemblies of the amphiphilic prodrug of gemcitabine might be a promising novel nanomedicine for targeted therapy of liver cancer.