Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, P. R. China.
University of Science and Technology of China, Hefei, 230026, P. R. China.
Small. 2021 May;17(19):e2008125. doi: 10.1002/smll.202008125. Epub 2021 Mar 24.
Photodynamic therapy is a new type of anti-tumor therapy with excellent therapeutic effects and minor side effects. The key factor for photodynamic therapy is highly efficient loading and protection of photosensitizers. Covalent organic framework is a new type of organic porous material with rich sources and has huge development potential in the loading of photosensitizers. However, the π-π interaction between the rigid monomers inevitably causes aggregation and quenching between photosensitizers, which in turn affects the rate of reactive oxygen production. Here, newly designed cationic flexible organic framework nanoparticles (PEI-Por NPs) are synthesized via one-step method with PEI25K and meso-tetra(p-formylphenyl)porphyrin under microwave irradiation. The structure of the flexible organic framework can effectively inhibit the aggregation and quenching of porphyrin. In addition, PEI-Por NPs had excellent gene transfection ability both in vitro and in vivo. Excellent antitumor effect can be achieved by combining PEI-Por NPs' photodynamic therapy capacity and PEI-Por NPs-mediated PD-L1 gene silencing with the guidance of fluorescence imaging and photoacoustic imaging. This cationic flexible organic framework material combines the advantages of flexible building units and rigid monomers, which provides a basis for the development of nano-photosensitizers and excellent gene carriers, and has great potential for clinical application.
光动力疗法是一种新型的抗肿瘤治疗方法，具有良好的治疗效果和较小的副作用。光动力疗法的关键因素是高效负载和保护光敏剂。共价有机骨架是一种新型的有机多孔材料，来源丰富，在光敏剂的负载方面具有巨大的发展潜力。然而，刚性单体之间的π-π相互作用不可避免地导致光敏剂之间的聚集和猝灭，从而影响活性氧的产生速率。在这里，通过微波辐射，以 PEI25K 和间四(对甲酰基苯基)卟啉为原料，通过一步法合成了新设计的阳离子柔性有机骨架纳米粒子（PEI-Por NPs）。柔性有机骨架的结构可以有效地抑制卟啉的聚集和猝灭。此外，PEI-Por NPs 在体外和体内均具有优异的基因转染能力。通过荧光成像和光声成像的指导，将 PEI-Por NPs 的光动力治疗能力与 PEI-Por NPs 介导的 PD-L1 基因沉默相结合，可实现优异的抗肿瘤效果。这种阳离子柔性有机骨架材料结合了柔性构筑单元和刚性单体的优点，为纳米光敏剂和优良基因载体的发展提供了基础，具有巨大的临床应用潜力。
