CAS Key Laboratory of Standardization and Measurement for Nanotechnology, CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology of China, Beijing 100190, PR China; University of Chinese Academy of Sciences, Beijing 100049, PR China.
CAS Key Laboratory of Standardization and Measurement for Nanotechnology, CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology of China, Beijing 100190, PR China.
Biomaterials. 2019 Jan;188:96-106. doi: 10.1016/j.biomaterials.2018.10.003. Epub 2018 Oct 9.
Mild acidity matrix, rich blood vessels and special biomarkers constitute the primary tumor microenvironment. Nanoparticles could change their physicochemical characteristics by functionalizing a series of moieties which is responsive towards pH or specific markers. So precise regulation of nanocarrier-based drug delivery systems by the tumor microenvironment has showed great potential for theranostics. Herein, we developed a smart nano delivery system STD-NM, showing tumor microenvironment responsive targeting, efficient drug delivery and precise evaluation of therapeutic effect in vivo. STD-NM kept in 'stealth' state in normal environment while 'activated' in the tumor acidic environment, which could show stability in blood circulation while deeply penetrate into tumor tissues. Additionally, STD-NM was designed with aggregation-induced emission (AIE) characteristic, of which the fluorescence 'switch on' when apoptosis taken place. Gene analysis by RNA-seq also confirmed a superior therapeutic effect of drug loaded STD-NM treatment. We envisioned the well-designed smart nano materials for drug delivery could open a new avenue in precisely tumor imaging and specific cancer therapeutics.
轻度酸性基质、丰富的血管和特殊的生物标志物构成了原发性肿瘤微环境。纳米粒子可以通过功能化一系列对 pH 值或特定标志物有响应的基团来改变其物理化学特性。因此，通过肿瘤微环境对基于纳米载体的药物传递系统进行精确调控，在治疗学上显示出了巨大的潜力。在本文中，我们开发了一种智能纳米递药系统 STD-NM，表现出肿瘤微环境响应靶向、高效药物传递和体内治疗效果的精确评估。STD-NM 在正常环境中保持“隐身”状态，而在肿瘤酸性环境中被“激活”，这使其在血液循环中保持稳定的同时，能够深入穿透肿瘤组织。此外，STD-NM 被设计为具有聚集诱导发射（AIE）特性，当发生细胞凋亡时，其荧光“开启”。通过 RNA-seq 的基因分析也证实了负载药物的 STD-NM 治疗的优越治疗效果。我们设想，精心设计的智能纳米材料用于药物输送，可以为精确的肿瘤成像和特定的癌症治疗开辟新途径。
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