Department of Polymer Science and Engineering and Key Laboratory of Systems Bioengineering of the Ministry of Education, School of Chemical Engineering and Technology, Tianjin University, Tianjin, 300072, China.
Tianjin Key Laboratory of Membrane Science and Desalination Technology, Tianjin University, Tianjin, 300072, China.
Macromol Rapid Commun. 2020 Feb;41(4):e1900570. doi: 10.1002/marc.201900570. Epub 2020 Jan 1.
Covalent organic frameworks (COFs) as drug delivery systems have shown great promise, but their pharmaceutical applications are often limited by complex building blocks, tedious preparations, irregular shape, and uncontrolled drug release within target cells. Herein, a facile strategy is developed to prepare PEGylated redox-responsive nanoscale COFs (denoted F68@SS-COFs) for efficiently loading and delivering doxorubicin (DOX) by use of FDA-approved Pluronic F68 and commercially available building blocks. The obtained F68@SS-COFs with controlled size, high stability, and good biocompatibility can not only achieve a very high DOX-loading content (about 21%) and very low premature leakage at physiological condition but can also rapidly respond to the tumor intracellular microenvironment and efficiently release DOX to kill tumor cells. Considering the readily available raw materials, simple preparation process, and desirable redox-responsiveness, the strategy provided here opens up a promising avenue to develop well-defined COFs-based nanomedicines for cancer therapy.
共价有机框架（COFs）作为药物传递系统具有很大的应用前景，但由于其复杂的结构单元、繁琐的制备过程、不规则的形状以及在靶细胞内不可控的药物释放等问题，其药物应用受到了限制。本文开发了一种简便的策略，使用 FDA 批准的聚乙二醇化的两亲性嵌段共聚物 Pluronic F68 和市售的构筑单元，制备了载药性能优异的 PEG 化氧化还原响应性纳米 COFs（记为 F68@SS-COFs）。所得的 F68@SS-COFs 具有尺寸可控、稳定性高、生物相容性好等优点，不仅可以实现高达 21%的载药率和极低的生理条件下的早期药物泄漏，而且可以快速响应肿瘤细胞内的微环境，并有效地释放 DOX 来杀伤肿瘤细胞。鉴于其易于获得的原料、简单的制备工艺和理想的氧化还原响应性，该策略为开发用于癌症治疗的具有明确结构的 COFs 基纳米药物提供了一条很有前途的途径。
