Nano-Micro Letters

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

Wei Shao1, #, Chuang Yang 1, 2, #, Fangyuan Li 1,*, Jiahe Wu 1,, Nan Wang 1, Qiang Ding 2, Jianqing Gao 1, Daishun Ling1, *

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Nano-Micro Lett. (2020) 12: 147

First Online: 13 July 2020 (Article)


*Corresponding author. E-mail: lfy@zju.edu.cn (F. L.), lingds@zju.edu.cn (D. L.)





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.



Molecular design; Isoindigo; Conjugated small molecule nanoparticles; Singlet-triplet energy gap; Synergistic PTT/PDT

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