Preparation And Bioactivity Study Of Platinum Drugs-Loaded Nanoparticles With Both Targeted And Intelligent Release Dual Functions

The main content of this paper is to construct platinum drugs-loaded nanoparticles with both targeted and intelligent release dual functions,and study the biological activity related to it.Specific work has the following two aspects.1.We successfully fabricated the well-defined folate-modified,cisplatin,ICG-loaded lipid-polymer hybrid nanoparticles(FCINPs)using a single-step sonication method.The FCINPs exhibited well-defined monodispersity,significant stability and excellent molecular targeting to FRs overexpressed on the surface of MCF-7 cells,and more importantly,this NPs not only retained the advantages of lipid-polymer hybrid NPs,but also had NIR-sensitivity and active targeting ability at the same time.The results demonstrated that the FCINPs have potential to be developed as an attractive drug delivery system against FRs overexpressed tumor cells.2.We successfully synthesized DSPE-PEG2000-Oct and fluorescent probe compounds(Probe 1),and fabricated the well-defined Octreotide-modified,cisplatin,Probe 1-loaded lipid-polymer hybrid nanoparticles(OCPNPs)using a single-step sonication method.The OCPNPs exhibited well-defined monodispersity,significant stability and smooth drug release rate.The cytotoxicity test and cell uptake experiments showed that this system has excellent octreotide targeting function and pH response and it can prevent the decrease in cisplatin activity caused by the combination of glutathione and cisplatin through specific binding of Probe 1 and glutathione in vivo.Combined with a variety of factors,We successfully improved the cell uptake efficiency and cisplatin anticancer activity of OCPNPs.