研究动态
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用于将青蒿素靶向黑色素瘤细胞的转铁蛋白缀合的纳米结构脂质载体。

Transferrin-Conjugated Nanostructured Lipid Carriers for Targeting Artemisone to Melanoma Cells.

发表日期:2024 Aug 22
作者: Njoud Altuwaijri, Eman Atef
来源: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

摘要:

我们报告了在转铁蛋白 (Tf) 缀合的纳米结构脂质载体 (NLC) 中成功配制青蒿素 (ATM),使细胞毒性增加了近五倍。新药研发成本不断上升,导致已批准的药物重新用于新的适应症。这项研究将抗疟药青蒿素融入纳米结构脂质载体 (NLC) 中,并测试了可能的抗癌作用。目的是开发 NLC 和封装青蒿素的转铁蛋白缀合 NLC (NLC-Tf),以增强其递送和抗癌活性。 NLC 制剂采用高压均质和超声处理制备,并通过粒径、zeta 电位和 PDI 进行表征。使用IR确认(Tf)与(NLC)的缀合,并使用MTS测定测试抗癌活性。所有配方均处于纳米尺寸范围(140-167 nm),具有不同的 zeta 电位值。红外光谱证实转铁蛋白与 NLC 成功缀合。使用 MTS 测定在黑色素瘤细胞系上测试制剂后,与阳性对照 ATM 相比,活力显着降低,封装的 ATM-Tf 毒性增加。 NLC 为将 ATM 递送至黑色素瘤细胞提供了一种有前途的潜在载体,并且与 Tf 的进一步结合显着提高了 ATM 的细胞毒性。
We report a successful formulation of Artemisone (ATM) in transferrin (Tf)-conjugated nanostructured lipid carriers (NLCs), achieving nearly a five-times increase in cell toxicity. The escalating cost of new drug discoveries led to the repurposing of approved drugs for new indications. This study incorporated Artemisone, an antimalarial drug, into a nanostructured lipid carrier (NLC) and tested for possible anticancer effects. The aim was to develop NLCs, and transferrin-conjugated NLCs (NLC-Tf) encapsulating Artemisone to enhance its delivery and anticancer activity. NLC formulations were prepared using high-pressure homogenization followed by ultrasonication and were characterized by particle size, zeta potential, and PDI. The conjugation of (Tf) to (NLC) was confirmed using IR, and the anticancer activity was tested using MTS assay. All formulations were in the nanometer size range (140-167 nm) with different zeta potential values. IR spectroscopy confirmed the successful conjugation of transferrin to NLC. Upon testing the formulations on melanoma cell lines using MTS assay, there was a significant decrease in viability and an increase in the encapsulated ATM-Tf toxicity compared to positive control ATM. The NLCs presented a promising potential carrier for delivering ATM to melanoma cells, and further conjugation with Tf significantly improved the ATM cytotoxicity.