Laboratory of Chemical Biology, State Key Laboratory of Rare Earth Resource Utilization, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, China; University of Chinese Academy of Sciences, Beijing, 100039, China.
Cancer Center, First Affiliated Hospital, Jilin University, Changchun, Jilin, 130061, PR China.
Biomaterials. 2019 Dec;223:119462. doi: 10.1016/j.biomaterials.2019.119462. Epub 2019 Aug 30.
Covalent organic frameworks (COFs) and their derivatives represent an emerging class of crystalline porous materials with broad potential applications. However, the biomedical applications of them were limited by the large size, low dispersivity, poor bioavailability within cells and metabolic problems. Herein, renal-clearable ultrasmall COF nanodots have been synthesized and utilized as efficient cancer therapy agents. A simple liquid exfoliation strategy was used to prepare COF nanodots. After polyethylene glycol (PEG) conjugation, the PEG coated COF nanodots (COF nanodots-PEG) showed improved physiological stability and biocompatibility. In addition, the well isolated porphyrin molecules endowed COF nanodots-PEG good light-triggered reactive oxygen species production ability, which showed excellent photodynamic therapy efficiency with good tumor accumulation ability. In particular, due to the ultrasmall size, COF nanodots-PEG could be cleared from the body through the renal filtration with no appreciable in vivo toxicity. Our study highlights the potential of COFs-based nanoparticles for biomedical applications.
共价有机骨架（COFs）及其衍生物是一类新兴的结晶多孔材料，具有广泛的潜在应用。然而，由于尺寸较大、分散性差、在细胞内的生物利用度低以及代谢问题等，它们在生物医学领域的应用受到限制。在此，我们合成了可经肾脏清除的超小 COF 纳米点，并将其用作有效的癌症治疗剂。我们采用简单的液相剥离策略来制备 COF 纳米点。经过聚乙二醇（PEG）修饰后，PEG 包裹的 COF 纳米点（COF 纳米点-PEG）具有更好的生理稳定性和生物相容性。此外，良好隔离的卟啉分子赋予 COF 纳米点-PEG 良好的光触发活性氧物质产生能力，其具有优异的光动力治疗效率和良好的肿瘤积累能力。特别地，由于其超小尺寸，COF 纳米点-PEG 可以通过肾脏过滤从体内清除，而体内无明显毒性。我们的研究强调了基于 COFs 的纳米粒子在生物医学应用中的潜力。
