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首页> 外文期刊>RSC Advances >Towards potent but less toxic nanopharmaceuticals – lipoic acid bioconjugates of ultrasmall gold nanoparticles with an anticancer drug and addressing unit
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Towards potent but less toxic nanopharmaceuticals – lipoic acid bioconjugates of ultrasmall gold nanoparticles with an anticancer drug and addressing unit

机译：迈向有效但毒性较小的纳米药物–超小金纳米颗粒的硫辛酸生物缀合物与抗癌药和寻址单元

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Modification of ultrasmall gold nanoparticles (AuNPs) with the lipoic acid derivative of folic acid was found to enhance their accumulation in the cancer cell, as compared to AuNPs without addressing units. The application of lipoic acid enabled the control of the gold nanoparticle functionalities leading to enhanced solubility and allowing for attachment of both the folic acid and the cytotoxic drug, doxorubicin. More robust attachment of doxorubicin to the nanoparticle through the amide bond resulted in toxicity comparable with that of the drug alone, opening a new perspective for designing more potent, but less toxic nanopharmaceuticals. The increased uptake was accompanied by pronounced nuclear accumulation and observable cytotoxicity. Doxorubicin binding via covalent amide bonds enhanced stability of the whole drug vehicle and provided much better control over doxorubicin release in the cell environment, as compared to physical adsorption or pH sensitive bonding commonly used for anthracycline carriers. Confocal microscopy revealed that the bond was stable in the cytoplasm for 22 h. The ability to slow down the rate of drug release may be crucial for the application in sustained anticancer drug delivery. Biological analyses performed using MTT assay and confocal microscopy confirmed that the ultrasmall AuNPs with the lipoic acid derivative of folic acid exhibit relatively low cytotoxicity, however when loaded with a chemotherapeutic, they cause a significant reduction in the cell viability.
机译：与没有寻址单元的AuNP相比，发现用叶酸的硫辛酸衍生物修饰超小金纳米颗粒（AuNPs）可增强其在癌细胞中的积累。硫辛酸的应用使得能够控制金纳米颗粒的功能性，从而导致溶解度提高，并允许叶酸和细胞毒性药物阿霉素的结合。阿霉素通过酰胺键更牢固地附着在纳米颗粒上，其毒性可与单独使用的药物相媲美，这为设计更有效，但毒性更低的纳米药物开辟了新的前景。摄取的增加伴随着明显的核积累和可观察到的细胞毒性。与通常用于蒽环类载体的物理吸附或pH敏感键相比，通过共价酰胺键进行的阿霉素结合增强了整个药物载体的稳定性，并更好地控制了细胞环境中阿霉素的释放。共聚焦显微镜显示该键在细胞质中稳定了22 h。减慢药物释放速率的能力对于持续抗癌药物递送中的应用可能至关重要。使用MTT分析和共聚焦显微镜进行的生物学分析证实，具有叶酸硫辛酸衍生物的超小AuNPs表现出相对较低的细胞毒性，但是，在进行化学治疗时，它们会导致细胞活力显着降低。

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