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首页> 外文期刊>RSC Advances >EGF-targeting lipodisks for specific delivery of poorly water-soluble anticancer agents to tumour cells
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EGF-targeting lipodisks for specific delivery of poorly water-soluble anticancer agents to tumour cells

机译：靶向EGF的脂质体可将水溶性较差的抗癌剂特异性递送至肿瘤细胞

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Concerns regarding poor aqueous solubility, high toxicity and lack of specificity impede the translation of many hydrophobic anticancer agents into safe and effective anticancer drugs. The application of colloidal drug delivery systems, and in particular the use of lipid-based nanocarriers, has been identified as a promising means to overcome these issues. PEG-stabilized lipid nanodisks (lipodisks) have lately emerged as a novel type of biocompatible, nontoxic and adaptable drug nanocarrier. In this study we have explored the potential of lipodisks as a platform for formulation and tumour targeted delivery of hydrophobic anticancer agents. Using curcumin as a model compound, we show that lipodisks can be loaded with substantial amounts of hydrophobic drugs (curcumin/lipid molar ratio 0.15). We demonstrate moreover that by deliberate choice of preparation protocols the lipodisks can be provided with relevant amounts of targeting proteins, such as epidermal growth factor (EGF). Data from in vitro cell studies verify that such EGF-decorated curcumin-loaded lipodisks are capable of EGF-receptor specific targeting of human A-431 tumour cells, and strongly suggest that the interaction between the lipodisks and the tumour cells results in receptor-mediated internalization of the disks and their cargo.
机译：关于水溶性差，高毒性和缺乏特异性的担忧阻碍了许多疏水性抗癌药向安全有效的抗癌药的转化。胶体药物递送系统的应用，尤其是基于脂质的纳米载体的使用，已被认为是克服这些问题的有希望的手段。 PEG稳定的脂质纳米盘（脂质盘）最近作为一种新型的生物相容性，无毒且适应性强的药物纳米载体出现。在这项研究中，我们探索了脂盘作为疏水性抗癌剂的制剂和肿瘤靶向递送平台的潜力。使用姜黄素作为模型化合物，我们显示脂质体可以装载大量疏水性药物（姜黄素/脂质摩尔比为0.15）。此外，我们证明通过精心选择制备方案，可以为脂片提供相关量的靶向蛋白，例如表皮生长因子（EGF）。来自体外细胞研究的数据证实，这种带有EGF修饰的姜黄素的脂质盘能够对人A-431肿瘤细胞进行EGF受体特异性靶向，并强烈暗示脂质盘与脂质体之间的相互作用肿瘤细胞导致受体介导的椎间盘及其货物内部化。

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