Preparation and Biocompatibility Evaluation of PEG-PLL/RGD-PEG-DSPE/Phospholipid/CaP Nanoparticles

(Arginine-Glycine-Aspartic)-methoxy polyethylene glycol-(1,2-distearoyl-sn-glycero-3-phosphoethanolaMine-N) (abbreviation: RGD-PEG₂₀₀₀-DSPE or RGD-PD) was successfully synthesized and verified by ¹H-NMR and MALDI-TOF MS. Polyethylene glycol-poly-L-lysine/RGD-PD/phospholipid/calcium phosphate nanoparticles (PEG-PLL/RGD-PD/PL/CaP NPs or MNPs) were prepared using a novel, simple method conducted at room temperature. Transmission electron microscopy (TEM) analysis showed that the MNPs were spheres of uniform size, with a diameter of ∼30 nm, and smooth surface. Thermogravimetric analysis (TGA) revealed that the PEG-PLL/RGD-PD/PL micelle was packed in the CaP shell. MNPs had little effect on hemolysis, coagulation, cardiac oxidative stress, inflammatory response and DNA damage, indicating negligible cytotoxicity in vitro and in vivo. Experiments in Zebrafish indicated that the MNPs neither affected the survival rate and heartbeat rate, nor induced malformation and apoptosis during embryogenesis. In conclusion, these results demonstrate that the newly-developed MNPs have good biocompatibility and a great potential as drug and gene carrier.