Pharmaceutical Sciences Department, MCPHS University, 179 Longwood Ave, Boston, MA 02115, USA.
Pharmacy College, West Coast University, 590 N Vermont Ave, Los Angeles, CA 90005, USA.
Int J Mol Sci. 2024 Aug 22;25(16):9119. doi: 10.3390/ijms25169119.
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.
我们成功地将青蒿素(ATM)制成转铁蛋白(Tf)缀合的纳米结构脂质载体(NLC),使细胞毒性增加近五倍。新药研发成本的不断上升导致人们开始重新利用已批准的药物来治疗新的适应症。本研究将抗疟药物青蒿素纳入纳米结构脂质载体(NLC)中,并测试其可能的抗癌作用。目的是开发纳米结构脂质载体(NLC)和转铁蛋白缀合的纳米结构脂质载体(NLC-Tf)来包裹青蒿素,以增强其递送和抗癌活性。使用高压匀质法随后进行超声处理来制备 NLC 制剂,并通过粒径、Zeta 电位和 PDI 进行表征。使用红外光谱(IR)确认(Tf)与(NLC)的缀合,使用 MTS 测定法测试抗癌活性。所有制剂的粒径均在纳米范围内(140-167nm),Zeta 电位值不同。IR 光谱证实转铁蛋白成功缀合到 NLC 上。通过 MTS 测定法在黑素瘤细胞系上测试这些制剂,与阳性对照 ATM 相比,细胞活力显著降低,包裹的 ATM-Tf 毒性增加。NLC 呈现出将 ATM 递送至黑素瘤细胞的有前途的载体,并且与 Tf 的进一步缀合显著提高了 ATM 的细胞毒性。