Preparation, Characterization And Vitro Evaluation Of Methotrexate-Phospholipid Complex Functionalized Graphene Oxide Nanohybrids

Nowdays,the application of anticancer drugs in chemotherapy was essential for cancer therapy.However,due to poor pharmacokinetics and nonspecific biodistribution,the traditional small-molecule drugs could easily lead to severe drug resistance,toxicity,and lack of intelligence in response to anticancer efficiency.To overcome these shortcomings,researchers have been developing continually drug delivery systems with a variety of improved efficiency such as safety,biocompatibility,and lower cytotoxicity.Therefore,we hypothesize that organic combination of methotrexate-phospholipid complex（MTX-SPC）with active targeting and carboxylated graphene oxide（CGO）with passive targeting as a drug delivery system,which could construct a kind of preparation with simple,multifunctional,and self-improve drug delivery system.The main work is as follow:（1）GO and CGO was prepared by an improved Hummers method.Then,GO and CGO were evaluated by ultraviolet-visible（UV-vis）,Fourier transform infrared spectroscopy（FT-IR）,X-ray diffractometry（XRD）,Scanning Electronic Microscopy（SEM）,and Dynamic light scattering（DLS）.（2）CGO/MTX-SPC nanohybrids were synthesized by non-covalent interactions using ultrasonic dispersion and solvent evaporation method.Then,CGO/MTX-SPC nanohybrids was characterized according to UV-vis,FT-IR,XRD,Transmission electron microscope（TEM）,Atomic force microscope（AFM）,DLS,and ELS.（3）In vitro cell study of CGO/MTX-SPC nanohybrids was evaluated on the basis of cellular uptake experiment,in vitro drug delivery,cell cytotoxicity assay,and the value of IC₅₀.The results dicates that CGO/MTX-SPC nanohybrids possess pH-dependent and sustained drug release behaviors,favorable biocompatibility,lower side effects,selectively target to cancer cells,and significantly higher cancer treatment effect.