Molecular Design of Conjugated Small Molecule Nanoparticles for Synergistically Enhanced PTT/PDT

Nano-Micro Letters

Chuang Yang¹  Fangyuan Li¹  Jianqing Gao¹  Wei Shao¹  Jiahe Wu¹  Nan Wang¹  Daishun Ling¹  Qiang Ding² 

[1] Institute of Pharmaceutics and Hangzhou Institute of Innovative Medicine, College of Pharmaceutical Sciences, Zhejiang University;Jiangsu Breast Disease Center, The First Affiliated Hospital with Nanjing Medical University;

关键词: Molecular design;    Isoindigo;    Conjugated small molecule nanoparticles;    Singlet–triplet energy gap;    Synergistic PTT/PDT;   

DOI  :  10.1007/s40820-020-00474-6

来源: DOAJ

【 摘 要 】

Abstract Simultaneous photothermal therapy (PTT) and photodynamic therapy (PDT) is beneficial for enhanced cancer therapy due to the synergistic effect. Conventional materials developed for synergistic PTT/PDT are generally multicomponent agents that need complicated preparation procedures and be activated by multiple laser sources. The emerging monocomponent diketopyrrolopyrrole (DPP)-based conjugated small molecular agents enable dual PTT/PDT under a single laser irradiation, but suffer from low singlet oxygen quantum yield, which severely restricts the therapeutic efficacy. Herein, we report acceptor-oriented molecular design of a donor–acceptor–donor (D–A–D) conjugated small molecule (IID-ThTPA)-based phototheranostic agent, with isoindigo (IID) as selective acceptor and triphenylamine (TPA) as donor. The strong D–A strength and narrow singlet–triplet energy gap endow IID-ThTPA nanoparticles (IID-ThTPA NPs) high mass extinction coefficient (18.2 L g−1 cm−1), competitive photothermal conversion efficiency (35.4%), and a dramatically enhanced singlet oxygen quantum yield (84.0%) comparing with previously reported monocomponent PTT/PDT agents. Such a high PTT/PDT performance of IID-ThTPA NPs achieved superior tumor cooperative eradicating capability in vitro and in vivo.

【 授权许可】

Unknown