title: Dual-targeting nanosystem for enhancing photodynamic therapy efficiency.
abstract: Photodynamic therapy (PDT) has been recognized as a valuable treatment option for localized cancers. Herein, we demonstrate a cellular and subcellular targeted strategy to facilitate PDT efficacy. The PDT system was fabricated by incorporating a cationic porphyrin derivative (MitoTPP) onto the polyethylene glycol (PEG)-functionalized and folic acid-modified nanographene oxide (NGO). For this PDT system, NGO serves as the carrier for MitoTPP as well as the quencher for MitoTPP's fluorescence and singlet oxygen ((1)O2) generation. Attaching a hydrophobic cation to the photosensitizer ensures its release from NGO at lower pH values as well as its mitochondria-targeting capability. Laser confocal microscope experiments demonstrate that this dual-targeted nanosystem could preferably enter the cancer cells overexpressed with folate receptor, and release its cargo MitoTPP, which subsequently accumulates in mitochondria. Upon light irradiation, the released MitoTPP molecules generate singlet oxygen and cause oxidant damage to the mitochondria. Cell viability assays suggest that the dual-targeted nanohybrids exhibit much higher cytotoxicity toward the FR-positive cells.
authors: College of Materials Science and Engineering, State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou 510640, China.
authors: Jiangsheng
authors: J
authors: Xu
authors: College of Materials Science and Engineering, State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou 510640, China.
authors: Fang
authors: F
authors: Zeng
authors: College of Materials Science and Engineering, State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou 510640, China.
authors: Hao
authors: H
authors: Wu
authors: College of Materials Science and Engineering, State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou 510640, China.
authors: Changmin
authors: C
authors: Yu
authors: College of Materials Science and Engineering, State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou 510640, China.
authors: Shuizhu
authors: S
authors: Wu
mesh_terms: D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D004058:Diffusion; D058973:Folate Receptors, GPI-Anchored / Q000378:metabolism; D005492:Folic Acid / Q000737:chemistry / Q000493:pharmacokinetics*; D006108:Graphite / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D008027:Light; D051379:Mice; D058990:Molecular Targeted Therapy / Q000379:methods; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D058726:Nanoconjugates / Q000008:administration & dosage / Q000737:chemistry / Q000648:ultrastructure; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D010087:Oxides; D010778:Photochemotherapy / Q000379:methods*; D017319:Photosensitizing Agents / Q000008:administration & dosage; D011166:Porphyrins / Q000008:administration & dosage* / Q000737:chemistry; D016896:Treatment Outcome
chemical_list: D058973:Folate Receptors, GPI-Anchored; D053769:Nanocapsules; D058726:Nanoconjugates; D010087:Oxides; D017319:Photosensitizing Agents; D011166:Porphyrins; D006108:Graphite; D005492:Folic Acid
keywords: drug delivery; dual-targeting; graphene oxide; mitochondria; photodynamic therapy