A Multifunctional Nanomicelle for Real-Time Targeted Imaging and Precise Near-Infrared Cancer Therapy

• Published in: Angewandte Chemie (International ed.) Vol. 53; no. 36; pp. 9544 - 9549
• Main Authors: Tian, Jiangwei, Ding, Lin, Ju, Huangxian, Yang, Yongchao, Li, Xilan, Shen, Zhen, Zhu, Zhi, Yu, Jun-Sheng, Yang, Chaoyong James
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 01.09.2014; WILEY‐VCH Verlag; Wiley; Wiley Subscription Services, Inc
• Edition: International ed. in English
• Subjects: Animals; Aptamers, Peptide - chemical synthesis; Aptamers, Peptide - therapeutic use; Boron Compounds; Cancer; Cancer therapies; Cell Line, Tumor; Chemistry; Chemistry, Multidisciplinary; Diagnostic Imaging; Effectiveness; Encapsulation; Fluorescence; fluorescence imaging; Fluorescent Dyes; Humans; Hydrogen-Ion Concentration; Imaging; Infrared Rays - therapeutic use; lysosome; Lysosomes; Lysosomes - pathology; Medical treatment; Mice; Micelles; Monitoring; Monitoring, Physiologic; Nanoparticles; Nanostructure; Neoplasms - diagnosis; Neoplasms - radiotherapy; photodynamic therapy; Photosensitizing Agents - chemical synthesis; Photosensitizing Agents - therapeutic use; Physical Sciences; Reactive Oxygen Species - chemistry; Real time; Science & Technology; therapeutic monitoring; Therapy; fluorescence imaging; photodynamic therapy; LIGHT; INDUCTION; AUTOPHAGY; CELL-DEATH; PROBES; CATHEPSINS; NANOPARTICLES; LYSOSOMES; therapeutic monitoring; cancer; APTAMERS; lysosome
• ISSN: 1433-7851; 1521-3773
• DOI: 10.1002/anie.201405490

Simultaneous targeted cancer imaging, therapy and real‐time therapeutic monitoring can prevent over‐ or undertreatment. This work describes the design of a multifunctional nanomicelle for recognition and precise near‐infrared (NIR) cancer therapy. The nanomicelle encapsulates a new pH‐activatable fluorescent probe and a robust NIR photosensitizer, R16FP, and is functionalized with a newly screened cancer‐specific aptamer for targeting viable cancer cells. The fluorescent probe can light up the lysosomes for real‐time imaging. Upon NIR irradiation, R16FP‐mediated generation of reactive oxygen species causes lysosomal destruction and subsequently trigger lysosomal cell death. Meanwhile the fluorescent probe can reflect the cellular status and in situ visualize the treatment process. This protocol can provide molecular information for precise therapy and therapeutic monitoring. All in one: A lysosome‐aimed multifunctional nanomicelle (Apt‐TNP) was developed by integrating a target‐cell‐specific aptamer, a pH‐activatable fluorescent probe, and a near‐infrared photosensitizer. Apt‐TNP enables simultaneous cancer imaging, photodynamic therapy, and real‐time self‐feedback of therapeutic efficacy.