merocyanine-dye and arginyl-glycyl-aspartic-acid

The application of photodynamic therapy in deep tissue is constrained by some pending problems, such as the limited penetration depth of excitation light and lacking of targeting ability. In this paper, a new kind of lipid coated upconverting nanoparticles consisiting of upconerting nanocrystal core and targeted lipid polymer shell was first reported for NIR triggered photodynamic therapy and cell imaging simultaneously. The lipid coated upconverting nanoparticles offers advantages to overcome the problem mentioned above. The UCN core works as a transducer to convert deeply penetrating near-infrared light to visible lights for activating photosensitizer and cell fluorescence imaging simultaneously. The amphiphilic lipid polymer RGD peptide conjugated poly (maleic anhydride-alt-1-octadecene) grafted dioleoyl l-α-phosphatidylethanolamine (RGD-PMAO-DOPE) acts as a shield. It can protect the system from catching by RES and target the whole system to the lesions. The experiment results show that the lipid coated upconverting nanoparticle is individual nanosphere with an average size of 20 nm. The drug loading can reach 9%. After NIR exposed, the MC540 was activated to produce singlet oxygen (ROS) successfully by the upconverting fluorescence emitted from UCN. Importantly, compared with nanoparticle without RGD decoration, the lipid coated upconverting nanoparticle can co-deliver the MC540 and UCNs into the same cell with higher efficiency. Besides, the MC540 loaded UCN/RGD-PMAO-DOPE nanoparticles showed significant inhibitory effect on tumor cells after NIR shining. Our data suggests that MC540 loaded UCN/RGD-PMAO-DOPE nanoparticle may be a useful nanoplatform for future PDT treatment in deep-cancer therapy.

Topics: Biological Transport; Cell Survival; Diagnostic Imaging; Drug Carriers; Humans; Infrared Rays; Maleic Anhydrides; MCF-7 Cells; Nanoparticles; Oligopeptides; Particle Size; Phosphatidylethanolamines; Photochemotherapy; Photosensitizing Agents; Pyrimidinones; Reactive Oxygen Species; Robotics; Spectroscopy, Fourier Transform Infrared