生育酚-人血清白蛋白纳米颗粒可增强拉帕替尼的给药效果，克服乳腺癌患者对多柔比星的耐药性。

Nanomedicine (London, England) Pub Date : 2024-07-02 DOI:10.1080/17435889.2024.2359357

Milan Paul, Sneha Das, Balaram Ghosh, Swati Biswas

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摘要

导言HER2是一种酪氨酸激酶受体，在HER2阳性乳腺癌中被扩增，驱动细胞信号传导和生长。目的：本研究旨在通过创建一种含有酪氨酸激酶抑制剂的纳米制剂疗法来对抗多药不敏感乳腺癌的多药耐药性。方法：将人血清白蛋白（HSA）与α-D-生育酚琥珀酸酯共轭，形成负载拉帕替尼（Lapa）的纳米聚集体。结果：生成的 Lapa@HSA(VE) NPs 大小为 117.2 nm，对 MCF7 (S) 和 MCF7 (R) 细胞株的 IC50 值分别为 10.25 μg/ml 和 8.02 μg/ml。结论与游离拉帕不同，拉帕@HSA(VE) NPs 在大鼠急性毒性研究中未显示出肝脏毒性。

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Tocopherol-human serum albumin nanoparticles enhance lapatinib delivery and overcome doxorubicin resistance in breast cancer.

Introduction: HER2, a tyrosine kinase receptor, is amplified in HER2-positive breast cancer, driving cell signaling and growth. Aim: This study aimed to combat multidrug resistance in Dox-insensitive breast adenocarcinoma by creating a nanoformulation therapy with a tyrosine kinase inhibitor. Methodology: Human serum albumin (HSA) was conjugated with α-D-tocopherol succinate to form nanoaggregates loaded with lapatinib (Lapa). Results: The resulting Lapa@HSA(VE) NPs were 117.2 nm in size and demonstrated IC50 values of 10.25 μg/ml on MCF7 (S) and 8.02 μg/ml on MCF7 (R) cell lines. Conclusion: Lapa@HSA(VE) NPs showed no hepatotoxicity, unlike free Lapa, as seen in acute toxicity studies in rats.

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Nanomedicine (London, England)

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