Precise Engineering of Multifunctional PEGylated Polyester Nanoparticles for Cancer Cell Targeting and Imaging

Multifunctional poly(ethylene glycol)-block-poly(lactic acid) (PEG-b-PLA) nanoparticles for cancer cell targeting and imaging have been designed by a combination of ring-opening polymerization and “click” chemistry. Nanoparticles containing both a targeting ligand and a fluorescent probe were prepared by blending PLA-b-PEG–ligand, PLA-b-PEG–fluorescent probe, and PLA-b-PEG–OMe copolymers at the molar ratios necessary to achieve the desired surface ligand and fluorescent probe densities. This strategy has been illustrated by the preparation of a large library of a variety of nanoparticles, such as ligand-decorated nanoparticles (with biotin, folic acid or anisamide), fluorescent nanoparticles (UV–vis or near-infrared dyes), and multifunctional nanoparticles decorated with a targeting ligand and a fluorescent probe. Successful targeting was demonstrated by surface plasmon resonance and in vitro experiments on different cancer cell lines.