This review covers the application of heptamethine cyanine dye (HMCD) mediated drug delivery. A relatively small number of HMCDs possess tumor targeting abilities, and this has spurred interest from research groups to explore them as drug delivery systems. Their tumor selectivity is primarily attributed to their uptake by certain isoforms of organic anion transporting polypeptides (OATPs) which are overexpressed in cancer tissues, although there are other possible mechanisms for the observed selectivity still under investigation. This specificity is confirmed using various cancer cell lines and is accompanied by moderate cytotoxicity. Their retention in tumor tissue is facilitated by the formation of albumin adducts as revealed by published mechanistic studies. HMCDs are also organelle selective dyes with specificity toward mitochondria and lysosomes, and with absorption and emission in the near-infrared region. This makes them valuable tools for biomedical imaging, especially in the field of fluorescence-guided tumor surgery. Furthermore, conjugating antitumor agents to HMCDs is providing novel drugs that await clinical testing. HMCD development as theranostic agents with dual tumor targeting and treatment capability signals a new approach to overcome drug resistance (mediated through evasion of efflux pumps) and systemic toxicity, the two parameters which have long plagued drug discovery.

中文翻译：

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七甲胺花青染料介导的药物递送：炒作或希望。

这篇综述涵盖了七甲胺花青染料（HMCD）介导的药物递送的应用。相对较少的HMCD具有靶向肿瘤的能力，这引起了研究小组的兴趣，将其探索为药物递送系统。它们的肿瘤选择性主要归因于它们在癌组织中过表达的某些有机阴离子转运多肽（OATP）异构体对它们的摄取，尽管尚有其他可能的机制可用于观察的选择性研究中。使用各种癌细胞系可以证实这种特异性，并伴有中等程度的细胞毒性。如已发表的机理研究所揭示的，白蛋白加合物的形成促进了它们在肿瘤组织中的保留。HMCD还是细胞器选择性染料，对线粒体和溶酶体具有特异性，并且在近红外区域具有吸收和发射。这使其成为用于生物医学成像的有价值的工具，尤其是在荧光引导的肿瘤手术领域。此外，将抗肿瘤剂与HMCD结合可提供等待临床测试的新型药物。HMCD作为具有双重肿瘤靶向和治疗能力的治疗药物的发展，标志着一种克服药物耐药性（通过逃逸外排泵的介导作用）和全身毒性的新方法，这两个参数长期困扰着药物的发现。将抗肿瘤剂与HMCD结合使用正在提供等待临床测试的新型药物。HMCD作为具有双重肿瘤靶向和治疗能力的治疗药物的发展，标志着一种克服药物耐药性（通过逃逸外排泵的介导作用）和全身毒性的新方法，这两个参数长期困扰着药物的发现。将抗肿瘤剂与HMCD结合使用正在提供等待临床测试的新型药物。HMCD作为具有双重肿瘤靶向和治疗能力的治疗药物的发展，标志着一种克服药物耐药性（通过逃逸外排泵的介导作用）和全身毒性的新方法，这两个参数长期困扰着药物的发现。