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Biodegradable Polymersomes with Structure Inherent Fluorescence and Targeting Capacity for Enhanced Photo‐Dynamic Therapy

Biodegradable nanostructures displaying aggregation‐induced emission (AIE) are desirable from a biomedical point of view, due to the advantageous features of loading capacity, emission brightness, and fluorescence stability. Herein, biodegradable polymers comprising poly (ethylene glycol)‐block‐poly...

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Published in:Angewandte Chemie International Edition 2021-08, Vol.60 (32), p.17629-17637
Main Authors: Cao, Shoupeng, Xia, Yifeng, Shao, Jingxin, Guo, Beibei, Dong, Yangyang, Pijpers, Imke A. B., Zhong, Zhiyuan, Meng, Fenghua, Abdelmohsen, Loai K. E. A., Williams, David S., Hest, Jan C. M.
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Language:English
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Summary:Biodegradable nanostructures displaying aggregation‐induced emission (AIE) are desirable from a biomedical point of view, due to the advantageous features of loading capacity, emission brightness, and fluorescence stability. Herein, biodegradable polymers comprising poly (ethylene glycol)‐block‐poly(caprolactone‐gradient‐trimethylene carbonate) (PEG‐P(CLgTMC)), with tetraphenylethylene pyridinium‐TMC (PAIE) side chains have been developed, which self‐assembled into well‐defined polymersomes. The resultant AIEgenic polymersomes are intrinsically fluorescent delivery vehicles. The presence of the pyridinium moiety endows the polymersomes with mitochondrial targeting ability, which improves the efficiency of co‐encapsulated photosensitizers and improves therapeutic index against cancer cells both in vitro and in vivo. This contribution showcases the ability to engineer AIEgenic polymersomes with structure inherent fluorescence and targeting capacity for enhanced photodynamic therapy. Polymersomes with inherent aggregation‐induced emission are presented that have mitochondrial targeting capacity due to the presence of pyridinium groups. The AIEgenic polymersomes, upon encapsulation of photosensitizers, show efficient energy transfer to enable photodynamic therapy, which improves the therapeutic index against cancer cells both in vitro and in vivo.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.202105103