Paclitaxel (PTX) is one of the most potent cancer drugs; however, its low solubility and strong systemic side effects limit its clinical applications. To overcome these issues, new drug formulations and chemical modifications have been proposed. In this study, we present conjugation of PTX to hybrid collagen-cell penetrating peptide (COL-CPP) carriers. The peptide carrier is highly soluble and utilizes a unique stabilization strategy: folding into a triple helix. Here, we report the formation of PTX-COL-CPP prodrug that has similar drug potency as free PTX when tested in Jurkat (human T lymphocyte of acute T cell leukemia) cells but not in A549 (human epithelial of lung carcinoma) cells. Confocal images and flow cytometry show that this behavior originates from lower cellular uptake of COL-CPP and endosomal entrapment of the prodrug in A549, but not in Jurkat cells.

中文翻译：

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紫杉醇与杂肽载体的缀合和Jurkat和A549癌细胞系的生物学评估

紫杉醇（PTX）是最有效的抗癌药物之一。但是，其低溶解度和强烈的全身性副作用限制了其临床应用。为了克服这些问题，已经提出了新的药物制剂和化学修饰。在这项研究中，我们提出了PTX与胶原蛋白穿透肽（COL-CPP）杂合载体的缀合。肽载体高度可溶，并利用独特的稳定化策略：折叠成三重螺旋。在这里，我们报道了在Jurkat（急性T细胞白血病的人T淋巴细胞）细胞中测试的PTX-COL-CPP前药的形成与游离PTX相似，而在A549（肺癌的人类上皮细胞）中则没有。共聚焦图像和流式细胞仪显示，这种行为源自A549中较低的细胞对COL-CPP的吸收和前体的内体包埋，