Yuan Youyong, Liu Bin
Department of Chemical and Biomolecular Engineering , National University of Singapore , 4 Engineering Drive 4 , Singapore 117585 . Email:
Institute of Materials Research and Engineering , Agency for Science , Technology and Research (ASTAR) , 3 Research Link , Singapore 117602.
Chem Sci. 2017 Apr 1;8(4):2537-2546. doi: 10.1039/c6sc05421h. Epub 2017 Jan 18.
Drug delivery systems (DDSs) have been extensively studied as carriers to deliver small molecule chemo-drugs to tumors for cancer therapy. The therapeutic efficiency of chemo-drugs is crucially dependent on the effective drug concentrations in tumors and cancer cells. Novel DDSs that can simultaneously unveil drug distribution, drug release/activation behaviors and offer early evaluation of their therapeutic responses are highly desirable. Traditional fluorescent dye-labeled DDSs may suffer from notorious aggregation-caused quenching (ACQ) with limited sensitivity for bioimaging; in addition, the intrinsic fluorescence of these dyes requires careful selection of energy acceptor or quencher moieties for a light-up probe design, which complicates the development of self-reporting DDSs, especially the ones for reporting multiple processes. The recently emerged fluorogens with aggregation-induced emission characteristics (AIEgens) offer a straightforward solution to tackle this challenge. Thanks to the unique properties of AIEgens, new theranostic DDSs have been developed for simultaneous drug delivery and bioimaging with high signal to background ratio and multiple signal reporting capabilities. In this mini-review, we summarize the recent development of theranostic DDSs based on AIEgens for monitoring the drug distribution, drug activation and prediction of the therapeutic responses. Through illustration of their design principles and application examples, we hope to stimulate the interest in the design of more advanced theranostic DDSs for biomedical research.
药物递送系统（DDSs）作为将小分子化疗药物递送至肿瘤用于癌症治疗的载体，已得到广泛研究。化疗药物的治疗效果关键取决于肿瘤和癌细胞中的有效药物浓度。非常需要能够同时揭示药物分布、药物释放/激活行为并对其治疗反应进行早期评估的新型DDSs。传统的荧光染料标记的DDSs可能会遭受臭名昭著的聚集诱导猝灭（ACQ），对生物成像的灵敏度有限；此外，这些染料的固有荧光需要为点亮探针设计仔细选择能量受体或猝灭剂部分，这使自报告DDSs的开发变得复杂，尤其是用于报告多个过程的DDSs。最近出现的具有聚集诱导发光特性的荧光团（AIEgens）为应对这一挑战提供了直接的解决方案。由于AIEgens的独特性质，已开发出新型的治疗诊断一体化DDSs，用于同时进行药物递送和生物成像，具有高信噪比和多信号报告能力。在本综述中，我们总结了基于AIEgens的治疗诊断一体化DDSs在监测药物分布、药物激活和治疗反应预测方面的最新进展。通过阐述其设计原理和应用实例，我们希望激发人们对设计更先进的治疗诊断一体化DDSs用于生物医学研究的兴趣。
