Jeong Keunsoo, Lee Yong-Deok, Park Solji, Lee Eunjung, Lim Chang-Keun, Lee Kyung Eun, Jeon Hyesung, Kim Jungahn, Chan Kwon Ick, Park Chong Rae, Kim Sehoon
Center for Theragnosis, Korea Institute of Science and Technology, 39-1 Hawolgok-dong, Seongbuk-gu, Seoul 136-791, Korea.
J Mater Chem B. 2013 Jul 28;1(28):3437-3442. doi: 10.1039/c3tb20387e. Epub 2013 Jun 3.
Hydrogen bonding is a major intermolecular interaction for self-assembly occurring in nature. Here we report novel polymeric carbohydrates, i.e., poly(oxyethylene galactaramide)s (PEGAs), as biomimetic building blocks to construct hydrogen bond-mediated self-assembled nanoparticles that are useful for biomedical in vivo applications. PEGAs were conceptually designed as a biocompatible hybrid between polysaccharide and poly(ethylene glycol) (PEG) to attain multivalent hydrogen bonding as well as fully hydrophilic, non-ionic and antifouling characteristics. It was revealed that PEGAs are capable of homospecies hydrogen bonding in water and constructing multi-chain assembled nanoparticles whose structural integrity is highly stable with varying concentration, temperature and pH. Using near-infrared fluorescence imaging we demonstrate facile blood circulation and efficient tumor accumulation of the self-assembled PEGA nanoparticles that were intravenously injected into mice. These in vivo behaviors elucidate the combined merits of our design strategy, i.e., biocompatible chemical constitution capable of multivalent hydrogen bonding, antifouling properties, minimal cell interaction and mesoscopic colloidal self-assembly, as well as size-motivated tumor targeting.
氢键是自然界中发生自组装的主要分子间相互作用。在此，我们报道了新型聚合物碳水化合物，即聚（氧乙烯半乳糖酰胺）（PEGA），作为仿生构建单元来构建氢键介导的自组装纳米颗粒，这些纳米颗粒可用于生物医学体内应用。PEGA在概念上被设计为多糖和聚乙二醇（PEG）之间的生物相容性杂化物，以实现多价氢键以及完全亲水、非离子和抗污特性。研究表明，PEGA能够在水中进行同种氢键作用，并构建多链组装纳米颗粒，其结构完整性在不同浓度、温度和pH值下高度稳定。通过近红外荧光成像，我们证明了静脉注射到小鼠体内的自组装PEGA纳米颗粒具有良好的血液循环和高效的肿瘤蓄积。这些体内行为阐明了我们设计策略的综合优点，即具有多价氢键作用的生物相容性化学组成、抗污性能、最小的细胞相互作用和介观胶体自组装，以及基于尺寸的肿瘤靶向性。
