Diacyllipid Micelle-Based Nanocarrier for Magnetically Guided Delivery of Drugs in Photodynamic Therapy

We report the design, synthesis using nanochemistry, and characterization of a novel multifunctional polymeric micelle-based nanocarrier system, which demonstrates combined function of magnetophoretically guided drug delivery together with light-activated photodynamic therapy. Specifically, the nanocarrier consists of polymeric micelles of diacylphospholipid-poly(ethylene glycol) (PE-PEG) coloaded with the photosensitizer drug 2-[1-hexyloxyethyl]-2-devinyl pyropheophorbide-a (HPPH), and magnetic Fe3O4 nanoparticles. The nanocarrier shows excellent stability and activity over several weeks. The physicochemical characterizations have been carried out by transmission electron micrography and optical spectroscopy. An efficient cellular uptake has been confirmed with confocal laser scanning microscopy. The loading efficiency of HPPH is practically unaffected upon coloading with the magnetic nanoparticles, and its phototoxicity is retained. The magnetic response of the nanocarriers was demonstrated by their magnetically directed delivery to tumor cells in vitro. The magnetophoretic control on the cellular uptake provides enhanced imaging and phototoxicity. These multifunctional nanocarriers demonstrate the exciting prospect offered by nanochemistry for targeting photodynamic therapy. Keywords: Photodynamic therapy; magnetic nanoparticles; polymeric micelles; magnetophoretic control of cellular uptake