分会

第二十八分会：超分子组装与软物质材料

摘要

近年来，癌症的发病率呈上升趋势，对人们的生命健康有着重大威胁。癌症的光热治疗是目前的一大研究热点，该方法具有微创、高效、时空可控性及能够抑制肿瘤转移等优势，是一种具有临床应用前景的癌症治疗方法。以纳米粒子为主体的新材料，是光热诊疗一体化研究最为活跃的领域。但金属纳米材料的代谢困难、碳基纳米材料诱导氧化应激、高分子纳米材料成药质量难以控制一直是有待解决的问题。 鉴于此，我们通过合理的分子设计，选用生物相容性优异的七甲川菁作为材料主链结构，通过调控分子间的相互作用，提出一种由非离子型有机小分子Cy7-TCF，在没有任何辅助分子的情况下通过超分子自组装的形式构建的具有生物功能的超分子纳米体系。超分子纳米片产生了明显的荧光自淬灭和独特的光热、光声成像特性。具有较高的光热转换效率（62.3%）和优异的光热稳定性。这些优势使其可以通过EPR效应被动靶向肿瘤后，可以通过近红外荧光成像和光声成像引导进行肿瘤光热治疗。最重要的是，超分子纳米片保留了有机小分子生物相容性好、生物安全性高的优势，不进入肿瘤位置的染料可以很快被肝脏清除。优异的光热性能及良好的生物安全性使该七甲川菁类超分子纳米体系有望成为未来癌症光热治疗的候选者。 Photothermal therapy Photothermal therapy (PTT) is a promising and elegant therapeutic means against tumors due to inherent advantages of minimum invasiveness, high-efficiency, space-time controllability and inhibition of tumor metastasis. Considerable effort has been devoted to develop more efficient PTT agents, especially the nanomaterials. However, the long-term toxicity of metal nanomaterials, the oxidative stress caused by carbon-based nanomaterials and difficulties in pharmaceutical-scale production of polymer nanomaterials underscore the challenges facing this field. In contrast, supramolecular nanomaterials, which use supramolecular design to improve the precision and effectiveness of pharmaceutical practice and optimize pharmacokinetic profiles, have gathered momentum to battle cancer and other incurable diseases, for which traditional small-molecular and macromolecular drugs are less effective. Here, we designed and synthetized a series of near-infrared supramolecular assembly-based nanodiscs which exhibit fluorescence self-quenching but unique photothermal properties with a high photothermal-conversion efficiency of 62.3%. After the nanodiscs passively targeting tumors by EPR effect, tumors can not only be monitored by near-infrared fluorescence imaging and photoacoustic tomography, but also be ablated by photothermal therapy under the irradiation. Due to the natural small organic molecules, these supramolecular assembly-based medicine have not been shown to be acute toxicity in vivo and can be eliminated by the liver, which exhibits excellent bio-compatibility and bio-safety. These supramolecular assembly-based medicine, which belong to the category of supramolecular drugs, can represent a new paradigm in drug delivery as single-component supramolecular medicine that is self-delivering and self-formulating and provides a platform technology for clinical cancer imaging and therapy.

关键词

超分子纳米片；自组装；近红外；多模态成像；光热治疗

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