Department of Chemical and Biomolecular Engineering, National University of Singapore, 4 Engineering Drive 4, 117585, Singapore, Singapore.
State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials, Ministry of Education and College of Life Sciences, Nankai University, Tianjin, 300071, China.
Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16396-16400. doi: 10.1002/anie.201809641. Epub 2018 Nov 14.
Liposomes have been used as popular drug delivery systems for cancer therapy. However, it is difficult to track traditional liposome delivery systems in an efficient and stable fashion to assess their delivery efficacy and biodistribution after administration. Meanwhile, conventional fluorescent liposomes containing optical tracers face the challenge of aggregation-caused quenching. Herein, we report a strategy for the integration of an aggregation-induced emission fluorogen with a liposome to yield an AIEgen-lipid conjugate, termed "AIEsome". The AIEsome exhibits bright red fluorescence along with great photostability and biocompatibility, and can be used for in vitro cancer cell labeling and in vivo tumor targeting. Meanwhile, benefiting from the excellent photosensitizing ability of the AIEgen and its good oxygen exposure in aqueous media, the AIEsome also performs well in efficient photodynamic therapy (PDT) for both in vitro cancer cell ablation and in vivo antitumor therapy after white light illumination.
脂质体已被用作癌症治疗的热门药物递送系统。然而,传统的脂质体递送系统难以高效且稳定地追踪,以评估其给药后的递送效果和生物分布。同时,含有光学示踪剂的传统荧光脂质体面临聚集诱导猝灭的挑战。在此,我们报告了一种将聚集诱导发射荧光团与脂质体整合的策略,得到一种称为“聚集诱导发光脂质体(AIEsome)”的 AIEgen-脂质缀合物。AIEsome 呈现明亮的红色荧光,同时具有出色的光稳定性和生物相容性,可用于体外癌细胞标记和体内肿瘤靶向。同时,得益于 AIEgen 的优异光动力治疗(PDT)能力及其在水相介质中的良好氧气暴露,AIEsome 在白光照射后进行的体外癌细胞消融和体内抗肿瘤治疗中也表现出良好的效果。