title: Relighting Photosensitizers by Synergistic Integration of Albumin and Perfluorocarbon for Enhanced Photodynamic Therapy.
abstract: Photodynamic therapy (PDT) is hampered by poor water solubility and skin phototoxicity of photosensitizers (PSs). Incorporation of PSs into nanocarrier (Nano-PDT) has been designed to overcome these problems. However, self-quenching of PSs highly condensed in Nano-PDT significantly reduced singlet oxygen (1O2) generation, resulting in unsatisfactory PDT efficacy. Here, we developed a novel tripleffect Nano-PDT, which has a special core-shell nanostructure by synergistic integration of perfluorotributylamine (PFTBA) and human serum albumin (HSA) to improve PDT. It has three mechanisms to relight quenched PSs, thereby generating more1O2. First, PSs uniformly dispersed in the shell, preventing self-quenching caused by π-π stacking. Second, HSA as nanocarrier extends the triplet-state lifetimes of PSs, increasing the amount of1O2. Third, PFTBA as core dissolves and protects1O2to extend the duration time of action of1O2. Compared with PS-encapsulated Nano-PDT, the self-quenching of PSs in tripleffect Nano-PDT can be effectively overcome. The fluorescence and1O2generation of PS are increased by approximately 100-fold and 15-fold, respectively. After intravenous injection into tumor-bearing mice, the tumor growth is significantly inhibited, while the PS-encapsulated Nano-PDT has almost no effect. The novel tripleffect Nano-PDT may guide improvement of existing clinical PDT and future PDT design.
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Medical School of Nanjing University , Nanjing 210093, China.
authors.forename: Hao
authors.initials: H
authors.lastname: Ren
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Medical School of Nanjing University , Nanjing 210093, China.
authors.forename: Jiaqi
authors.initials: J
authors.lastname: Liu
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Medical School of Nanjing University , Nanjing 210093, China.
authors.forename: Fenhong
authors.initials: F
authors.lastname: Su
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Medical School of Nanjing University , Nanjing 210093, China.
authors.forename: Sizhan
authors.initials: S
authors.lastname: Ge
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Medical School of Nanjing University , Nanjing 210093, China.|State Key Laboratory of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.|Jiangsu Key Laboratory for Nano Technology, Nanjing University , Nanjing 210093, China.|Institute of Drug R&D, Medical School of Nanjing University , Nanjing 210093, China.|Jiangsu R&D Platform for Controlled & Targeted Drug Delivery, Nanjing University , Nanjing 210093, China.
authors.forename: Ahu
authors.initials: A
authors.lastname: Yuan
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Medical School of Nanjing University , Nanjing 210093, China.
authors.forename: Weimin
authors.initials: W
authors.lastname: Dai
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Medical School of Nanjing University , Nanjing 210093, China.|State Key Laboratory of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.|Jiangsu Key Laboratory for Nano Technology, Nanjing University , Nanjing 210093, China.|Institute of Drug R&D, Medical School of Nanjing University , Nanjing 210093, China.|Jiangsu R&D Platform for Controlled & Targeted Drug Delivery, Nanjing University , Nanjing 210093, China.
authors.forename: Jinhui
authors.identifier: http://orcid.org/0000-0003-3087-7367
authors.initials: J
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Medical School of Nanjing University , Nanjing 210093, China.|State Key Laboratory of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.|Jiangsu Key Laboratory for Nano Technology, Nanjing University , Nanjing 210093, China.|Institute of Drug R&D, Medical School of Nanjing University , Nanjing 210093, China.|Jiangsu R&D Platform for Controlled & Targeted Drug Delivery, Nanjing University , Nanjing 210093, China.
authors.forename: Yiqiao
authors.initials: Y
authors.lastname: Hu
mesh_terms: D000418:Albumins; D000818:Animals; D005466:Fluorocarbons; D006801:Humans; D051379:Mice; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000737:chemistry*; D026082:Singlet Oxygen
chemical_list: D000418:Albumins; D005466:Fluorocarbons; D017319:Photosensitizing Agents; D026082:Singlet Oxygen
keywords: core−shell structure; human serum albumin; perfluorocarbon; photodynamic therapy; self-quenching; tripleffect