Porphyrins are organic heterocyclic macrocycles with photophysical properties well-suited for clinical phototherapy and cancer imaging. However, their wider application in the clinical management of disease is barred by poor aqueous solubility, bioavailability, tumour accumulation and skin phototoxicity. These limitations instigated the development of supramolecular platforms that improved porphyrin pharmacokinetics and tumour-homing. The supramolecular formulation of porphyrins also facilitates single agent-mediated deeper tissue photoactivation, extended imaging and theranostic multimodality, and synergistic application of multiple therapies. Supramolecular porphyrin structures can overcome additional limitations of porphyrin-mediated photodynamic therapy (PDT), including low depths of tissue penetration that restrict PDT to superficial lesions, inability to treat hypoxic tumours, and incomplete tumour damage. In this review, we discuss the photophysical properties of porphyrins, and overview the clinically-relevant advantages and challenges arising from their incorporation within supramolecular platforms. Specifically, fundamentals underlying the ability of these platforms to ameliorate passive and active porphyrin delivery to tumours, achieve deeper tissue PDT via red-shifted porphyrin Q-bands, energy transfer and sonodynamic effects, and enable new porphyrin-mediated theranostics and synergistic therapeutic capabilities will be explained and exemplified with seminal and cutting-edge in vivo studies.

中文翻译：

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通过超分子化学提高卟啉的生物医学实用性

卟啉是具有光物理性质的有机杂环大环化合物，非常适合临床光疗和癌症成像。但是，由于水溶性差，生物利用度，肿瘤蓄积和皮肤光毒性差，它们在疾病的临床管理中的广泛应用受到禁止。这些局限性促使超分子平台的发展，该平台改善了卟啉的药代动力学和肿瘤归巢。卟啉的超分子制剂还促进了单药介导的更深层组织的光活化，扩展的成像和治疗诊断的多模态性以及多种疗法的协同应用。超分子卟啉结构可以克服卟啉介导的光动力疗法（PDT）的其他局限性，包括组织渗透深度低，将PDT限制在浅表性病变，无法治疗缺氧性肿瘤和不完全的肿瘤损害。在这篇综述中，我们讨论了卟啉的光物理性质，并概述了由于它们掺入超分子平台而产生的临床相关优势和挑战。具体而言，这些平台改善被动和主动卟啉传递至肿瘤，实现更深层组织PDT的能力的基础通过红移的卟啉Q波段，能量转移和声动力学效应，并启用新的卟啉介导的治疗学和协同治疗功能，将以开创性和前沿的体内研究为例进行说明和举例说明。