Department of Organic Chemistry, Universidad Autónoma de Madrid, Institute for Advanced Research in Chemical Sciences, Calle Francisco Tomás y Valiente, 7, 28049 Madrid, ES, Spain.
IMDEA Nanociencia, c/Faraday 9, Cantoblanco, 28049, ES, Spain.
Biomater Sci. 2022 Jun 14;10(12):3259-3267. doi: 10.1039/d2bm00173j.
Photodynamic therapy (PDT) represents a promising treatment modality for a range of cancers and other non-malignant diseases due to its non-invasive nature arising from the light-dependent activation. However, PDT has not been the first-line treatment of cancer thus far as a consequence of, among others, the lack of effective transport and activation strategies, and the undesired side effect caused by skin photosensitisation induced by the "always on" photosensitisers. To overcome this "Achilles' heel", we present herein a non-covalent approach to construct a one-component dynamic supramolecular nanophotosensitising system based on a carefully designed porphyrin. The control of the photoactivities of the resulting supramolecular fibres lies in the spatiotemporal control of the monomer-polymer equilibrium. Both the thermodynamics and kinetics of this nanosystem have been carefully studied by different techniques. Moreover, and studies have also been performed, showing that these supramolecular aggregates exhibit facile cell internalisation and progressive disassembly after being endocyted by targeted cells, leading to activation of the photosensitising units and eventually cell death and tumour eradication under photoirradiation.
光动力疗法（PDT）由于其基于光依赖性激活的非侵入性特性，代表了一系列癌症和其他非恶性疾病的有前途的治疗方式。然而，由于缺乏有效的传输和激活策略，以及由“始终开启”光敏剂引起的皮肤光致敏引起的不期望的副作用，PDT 迄今为止尚未成为癌症的一线治疗方法。为了克服这一“阿喀琉斯之踵”，我们在此提出了一种非共价方法，基于精心设计的卟啉构建了一种单一组分的动态超分子纳米光敏化系统。所得超分子纤维光活性的控制在于单体-聚合物平衡的时空控制。通过不同的技术，仔细研究了这个纳米系统的热力学和动力学。此外，还进行了 和 研究，表明这些超分子聚集体在被靶向细胞内吞后表现出易于细胞内化和渐进解体，导致光敏化单元的激活，并最终在光照射下导致细胞死亡和肿瘤消除。
