J‐Aggregate‐Based FRET Monitoring of Drug Release from Polymer Nanoparticles with High Drug Loading

• Published in: Angewandte Chemie International Edition 2020-11, Vol.59 (45), p.20065-20074
• Main Authors: Liu, Yun, Yang, Guangze, Jin, Song, Zhang, Run, Chen, Peng, Tengjisi, Wang, Lianzhou, Chen, Dong, Weitz, David A., Zhao, Chun‐Xia
• Format: Article
• Language: English
• Subjects: Aggregates; Drug Carriers - chemistry; Drug delivery; Drug delivery systems; Drug Liberation; drug release; Dyes; Fluorescence; Fluorescence resonance energy transfer; Fluorescence Resonance Energy Transfer - methods; FRET; J-aggregates; Kinetics; Microscopy, Electron, Transmission; Nanoparticles; Nanoparticles - chemistry; Polymers; Polymers - chemistry
• ISSN: 1433-7851; 1521-3773
• DOI: 10.1002/anie.202008018

Understanding drug‐release kinetics is critical for the development of drug‐loaded nanoparticles. We developed a J‐aggregate‐based Förster‐resonance energy‐transfer (FRET) method to investigate the release of novel high‐drug‐loading (50 wt %) nanoparticles in comparison with low‐drug‐loading (0.5 wt %) nanoparticles. Single‐dye‐loaded nanoparticles form J‐aggregates because of the high dye‐loading (50 wt %), resulting in a large red‐shift (≈110 nm) in the fluorescence spectrum. Dual‐dye‐loaded nanoparticles with high dye‐loading using FRET pairs exhibited not only FRET but also a J‐aggregate red‐shift (116 nm). Using this J‐aggregate‐based FRET method, dye‐core–polymer‐shell nanoparticles showed two release processes intracellularly: the dissolution of the dye aggregates into dye molecules and the release of the dye molecules from the polymer shell. Also, the high‐dye‐loading nanoparticles (50 wt %) exhibited a slow release kinetics in serum and relatively quick release in cells, demonstrating their great potential in drug delivery. A J‐aggregate‐based Förster‐resonance energy‐transfer (FRET) method to investigate the release of high‐drug‐loading (50 wt %) and low‐drug‐loading (0.5 wt %) nanoparticles is reported. The high‐dye‐loading nanoparticles exhibited a slow release kinetics in serum and a relatively quick release in cells, demonstrating their great potential in drug delivery.