Introduction: Synergistic treatment integrating photothermal therapy (PTT) and chemotherapy is a promising strategy for hepatocellular carcinoma (HCC). However, the most commonly used photothermal agent, IR820, and chemotherapeutic drug, doxorubicin hydrochloride (DOX), are both hydrophilic molecules that suffer from the drawbacks of a short circulation time, rapid elimination and off-target effects.
Methods and Results: Herein, a novel nanodrug that combined HCC-targeted IR820 and DOX was developed based on excipient-free co-assembly. First, lactosylated IR820 (LA-IR820) was designed to target HCC. Then, the LA-IR820/DOX nanodrug (LA-IR820/DOX ND) was purely self-assembled without excipient assistance. The physicochemical properties and the chemo-photothermal antitumour activity of the excipient-free LA-IR820/DOX ND were evaluated. More importantly, the obtained LA-IR820/DOX ND exhibited 100% drug loading, remarkable HCC targeting and excellent antitumour efficacy.
Conclusion: This excipient-free LA-IR820/DOX ND may be a promising candidate for the synchronous delivery and synergistic targeting of IR820 and DOX as a combined chemo-photothermal therapy.

Keywords: excipient-free, hepatoma cell targeting, self-assembly nanodrug, photothermal therapy, chemotherapy




中文翻译：

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用于协同抗肿瘤治疗的乳糖基化 IR820/DOX 共组装纳米药物。

简介：光热疗法（PTT）和化学疗法相结合的协同治疗是治疗肝细胞癌（HCC）的一种有前景的策略。然而，最常用的光热剂IR820和化疗药物盐酸阿霉素（DOX）均为亲水性分子，存在循环时间短、消除快、脱靶等缺点。
方法和结果：在此，基于无赋形剂共组装开发了一种结合 HCC 靶向 IR820 和 DOX 的新型纳米药物。首先，乳糖基化 IR820 (LA-IR820) 旨在靶向 HCC。然后，LA-IR820/DOX 纳米药物（LA-IR820/DOX ND）在没有辅料辅助的情况下完全自组装。评估了不含赋形剂的 LA-IR820/DOX ND 的理化性质和化学光热抗肿瘤活性。更重要的是，获得的 LA-IR820/DOX ND 具有 100% 的载药量、显着的 HCC 靶向性和优异的抗肿瘤功效。
结论：这种不含赋形剂的 LA-IR820/DOX ND 可能是 IR820 和 DOX 作为联合化学光热疗法同步递送和协同靶向的有希望的候选者。

关键词：无赋形剂, 肝癌细胞靶向, 自组装纳米药物, 光热疗法, 化疗