Nanoparticle-based biomedicine has received enormous attention for theranostic applications, as these systems are expected to overcome several drawbacks of conventional therapy. Herein, effective and controlled drug delivery systems with on-demand release abilities and biocompatible properties are used as a versatile and powerful class of nanocarriers. We report the synthesis of a novel biocompatible and multifunctional material, entirely consisting of covalently crosslinked organic molecules. Specifically, β-cyclodextrin (CD) precursors were crosslinked with rigid organic linker molecules to obtain small (∼150 nm), thermally stable and highly water-dispersible nanoparticles with an accessible pore system containing β-CD rings. The nanoparticles can be covalently labeled with dye molecules to allow effective tracking in in vitro cell experiments. Rapid sugar-mediated cell-uptake kinetics were observed with HeLa cells, revealing exceptional particle uptake within only 30 minutes. Additionally, the particles could be loaded with different cargo molecules showing pH-responsive release behavior. Successful nuclei staining with Hoechst 33342 dye and effective cell killing with doxorubicin cargo molecules were demonstrated in live-cell experiments, respectively. This novel nanocarrier concept provides a promising platform for the development of controllable and highly biocompatible theranostic systems.

中文翻译：

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生物相容性交联的β-环糊精纳米颗粒可作为多功能载体用于细胞递送†

基于纳米颗粒的生物医学在治疗学应用中受到了极大的关注，因为这些系统有望克服常规疗法的一些缺点。在本文中，具有按需释放能力和生物相容性的有效和受控的药物递送系统被用作一类通用且功能强大的纳米载体。我们报告了一种新型的生物相容性和多功能材料的合成，该材料完全由共价交联的有机分子组成。具体而言，将β-环糊精（CD）前体与刚性有机连接剂分子交联，以获得较小的（〜150 nm），热稳定且高度水分散性的纳米颗粒，且该纳米颗粒具有可触及的包含β-CD环的孔系统。纳米颗粒可以用染料分子共价标记，以有效跟踪体外细胞实验。用HeLa细胞观察到快速的糖介导的细胞摄取动力学，揭示了仅30分钟内异常的颗粒摄取。另外，颗粒可以负载有显示pH响应释放行为的不同货物分子。分别在活细胞实验中证明了用Hoechst 33342染料成功进行的核染色和用阿霉素货物分子对细胞的有效杀伤。这种新颖的纳米载体概念为可控和高度生物相容性治疗学系统的开发提供了一个有前途的平台。