Biodegradable and crosslinkable PPF-PLGA-PEG self-assembled nanoparticles dual-decorated with folic acid ligands and Rhodamine B fluorescent probes for targeted cancer imaging

Novel biodegradable and crosslinkable copolymers of hydrophobic poly(propylene fumarate)-co-poly(lactic-co-glycolic acid) (PPF-PLGA) linked with hydrophilic poly(ethylene glycol) (PEG), namely PPF-PLGA-PEG, were developed and fabricated into core-shell nanoparticles through self-assembly and photocrosslinking. A fluorescent probe, Rhodamine B (RhB), was conjugated to the end of the copolymer chain (PPF-PLGA-PEG-RhB), which allows tracking of the nanoparticles through visualizing the fluorescence probe. Folic acid (FA) ligand was conjugated to another series of chains (PPF-PLGA-PEG-FA) for targeted delivery of the nanoparticles to the tumor sites by binding to the ubiquitously overexpressed FA receptors on tumor cells. Our results showed that PPF-PLGA-PEG nanoparticles incorporated with RhB fluorescence probes and FA tumor binding ligands have specific cancer cell targeting and imaging abilities. These crosslinkable nanoparticles are potentially useful to serve as a platform for conjugation of fluorescence probes as well as various antibodies and peptides for cancer targeted imaging or drug delivery.