Targeted photodynamic-induced singlet oxygen production by peptide-conjugated biodegradable nanoparticles for treatment of skin melanoma.

摘要: Abstract Background Photodynamic therapy (PDT) has been determined to be a promising treatment modality in the most resistant tumors such as malignant melanoma. However, key cytotoxic agent of PDT, -singlet oxygen (1O2) - represents high risk photodynamic-associated side effects e.g. skin photosensitization. Recently, controllable photosensitization, where 1O2 is produced on demand, received increasing attention. In our study, this could achieved via loading photosensitizer (PS) nanoparticles (NPs) decorated with target-specific moieties characterized by quenching abilities specifically locate PS targeted cells and assure that only desired after cellular processing. Methods Polymeric hybrid lipid-polymer NPs were formulated assayed for their physicochemical properties. This was followed conjugation an active targeting ligand, cRGDyk, cyclic (Arginine-Glycine-Aspartic acid-D-Tyrosine-Lysine) peptide. Finally, photodynamic potential selected formulations quantification production vitro cytotoxicity. Results Three nominated choice (FOCs); FOC-1 (200 nm, polymeric), FOC-2 (130 nm, polymeric) FOC-3 hybrid). Physicochemical properties, importantly particle size NPs’ composition have shown major determinants PDT-mediated cytotoxicity Conclusion Proper selection intended PDT application ligands achieve dual targeting; enhanced accumulation protection elsewhere other than target cells.