State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , 5625 Renmin Street, Changchun, Jilin 130022, P. R. China.
University of Chinese Academy of Sciences , Beijing 100049, P. R. China.
ACS Appl Mater Interfaces. 2017 Sep 6;9(35):29612-29622. doi: 10.1021/acsami.7b10763. Epub 2017 Aug 24.
Polymeric nanoparticles (NPs) play a key role in nanoscale formulations for bioimaging, cancer treatment, and theranostics. In this work, we designed and synthesized a series of hydrophobic polymers (P1-6) with different pendent groups via one-step multicomponent Passerini reaction. These polymers possessed similar molecular structures and various biomedical functions. Interestingly, they could self-assemble into stable NPs in aqueous media. All formed NPs were redox sensitive because of the existence of disulfide bonds in the backbone. The stability of NPs in aqueous media with or without glutathione was systematically evaluated and compared. The optical performance, including fluorescence resonance energy transfer, was characterized under different conditions for those polymers with fluorescent components. Importantly, all formed NPs showed good cytocompatibility toward HeLa cells and different biological functions, including drug loading and delivery, bioimaging with variable fluorescence, and photodynamic activity, as evidenced by experiments in vitro and in vivo. These results demonstrate the great potential of multicomponent reaction to customize versatile polymeric nanoparticles for biomedical applications.
聚合物纳米粒子（NPs）在生物成像、癌症治疗和治疗学的纳米级制剂中起着关键作用。在这项工作中，我们通过一步多组分 Passerini 反应设计并合成了一系列具有不同侧基的疏水性聚合物（P1-6）。这些聚合物具有相似的分子结构和各种生物医学功能。有趣的是，它们可以在水介质中自组装成稳定的 NPs。由于骨架中存在二硫键，所有形成的 NPs 均具有氧化还原敏感性。系统评估和比较了 NPs 在含或不含谷胱甘肽的水介质中的稳定性。对具有荧光成分的聚合物在不同条件下的光学性能（包括荧光共振能量转移）进行了表征。重要的是，所有形成的 NPs 对 HeLa 细胞均表现出良好的细胞相容性，并具有不同的生物学功能，包括药物负载和递送、具有可变荧光的生物成像以及光动力活性，这一点通过体外和体内实验得到了证明。这些结果表明多组分反应在定制用于生物医学应用的多功能聚合物纳米粒子方面具有巨大的潜力。
