Abstract In this work, we investigated terpyridine (tpy)/Zn(II) complexation for the crosslinking of polymeric micelles of the branched poly(ethylene oxide)–poly(propylene oxide) block copolymer Tetronic® 1107 (T1107) in water and produce physically stable amphiphilic luminescent nanogels. Nanoparticles displayed a size of 235 ± 25 and 318 ± 57 nm before and after Zn(II) crosslinking, respectively, as measured by dynamic light scattering. High-resolution scanning electron microscopy analysis revealed the multimicellar nature of the crosslinked nanoparticles. In addition, Zn(II) complexation prevented nanoparticle disassembly after extreme dilution below the critical micellar concentration and reduced the minimum concentration required for the reverse thermal gelation of concentrated aqueous T1107 systems. The cell compatibility and uptake were initially assessed in the murine macrophage cell line RAW 264.7. Results showed that complexation increases the cell compatibility of the nanoparticles with respect to the non-complexed counterparts. In addition, non-crosslinked nanoparticles accumulated in the cell membrane, while the complexed ones were internalized, as observed by confocal laser scanning fluorescence microscopy. Then, the antiproliferative activity of the crosslinked nanoparticles was confirmed in the rhabdomyosarcoma cell line Rh30; their inhibitory concentration 50 (IC50) being 101 μg/mL (6.7 μM). Finally, the encapsulation and release of the hydrophobic antiretroviral efavirenz was characterized in vitro. Complexation slightly reduced the release kinetics with respect to the pristine nanoparticles. Overall results demonstrate the promise of this simple modification strategy to produce amphiphilic nanogels with a set of advantageous physicochemical, optical, and biological properties.

中文翻译：

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通过聚合物胶束的三联吡啶-Zn（II）络合发光两亲纳米凝胶

摘要 在这项工作中，我们研究了三联吡啶 (tpy)/Zn(II) 络合用于支化聚（环氧乙烷）-聚（环氧丙烷）嵌段共聚物 Tetronic® 1107 (T1107) 在水中的聚合物胶束的交联，并在水中物理产生稳定的两亲发光纳米凝胶。通过动态光散射测量，纳米颗粒在 Zn(II) 交联前后的尺寸分别为 235 ± 25 和 318 ± 57 nm。高分辨率扫描电子显微镜分析揭示了交联纳米粒子的多胶束性质。此外，在低于临界胶束浓度的极端稀释后，Zn(II) 络合可防止纳米颗粒解体，并降低了浓缩含水 T1107 系统反向热凝胶化所需的最低浓度。细胞相容性和吸收最初在鼠巨噬细胞系 RAW 264.7 中进行评估。结果表明络合增加了纳米颗粒相对于非络合对应物的细胞相容性。此外，通过共聚焦激光扫描荧光显微镜观察到，未交联的纳米颗粒在细胞膜中积累，而复合的纳米颗粒则被内化。然后，在横纹肌肉瘤细胞系Rh30中证实了交联纳米颗粒的抗增殖活性；它们的抑制浓度 50 (IC50) 为 101 μg/mL (6.7 μM)。最后，在体外表征了疏水性抗逆转录病毒依非韦伦的封装和释放。络合略微降低了原始纳米颗粒的释放动力学。