Koothradan Suhana, Nayeem Safia, Elyas K K
Department of Biotechnology, University of Calicut, Kerala Malappuram, 673635 India.
3 Biotech. 2025 Jan;15(1):23. doi: 10.1007/s13205-024-04189-y. Epub 2024 Dec 25.
Rapamycin analogs are approved by the FDA for breast and renal cancer treatment. Hence, the possibility of nanoparticle-mediated delivery of Rapamycin could be examined. In the present study, PEGylated Gold-core shell iron oxide nanoparticles were used for the targeted delivery of Rapamycin, and R-Au-IONPs were formulated. SEM, XRD, and FTIR determined the smooth spherical morphology, and compositional structure, and confirmed the conjugation of Rapamycin onto the NPs. The in vitro drug release study showed a controlled release of the drug over time. R-Au-IONPs showed significant cytotoxicity in MCF 7 cells. Anti-proliferative assays such as trypan blue dye exclusion assay, microscopy, Fluorescent staining, and clonogenic assays were performed. NH staining, Rhodamine 123 staining, PS externalization, and the cleavage of PARP protein by western immunoblot assays confirmed the induction of apoptosis. The mechanism of R-Au-IONP-induced cell death was analyzed by flow cytometry. Our in-vitro study, on the impact of R-Au-IONPs on cell viability in the human breast adenocarcinoma cell line (MCF-7), confirms the efficacy of drug delivery using the nanoparticle system. Further results implied the induction of apoptosis. This drug delivery system using Rapamycin could be a potential candidate in the treatment of breast cancer.
雷帕霉素类似物已获美国食品药品监督管理局（FDA）批准用于治疗乳腺癌和肾癌。因此，可以研究纳米颗粒介导递送雷帕霉素的可能性。在本研究中，聚乙二醇化的金核壳氧化铁纳米颗粒用于雷帕霉素的靶向递送，并制备了R-Au-IONPs。扫描电子显微镜（SEM）、X射线衍射（XRD）和傅里叶变换红外光谱（FTIR）确定了其光滑的球形形态、组成结构，并证实了雷帕霉素与纳米颗粒的缀合。体外药物释放研究表明药物随时间呈控释。R-Au-IONPs在MCF 7细胞中显示出显著的细胞毒性。进行了诸如台盼蓝染料排除试验、显微镜检查、荧光染色和克隆形成试验等抗增殖试验。通过NH染色、罗丹明123染色、磷脂酰丝氨酸（PS）外化以及蛋白质免疫印迹法检测聚腺苷二磷酸核糖聚合酶（PARP）蛋白的裂解，证实了细胞凋亡的诱导。通过流式细胞术分析了R-Au-IONP诱导细胞死亡的机制。我们关于R-Au-IONPs对人乳腺腺癌细胞系（MCF-7）细胞活力影响的体外研究，证实了使用纳米颗粒系统进行药物递送的有效性。进一步的结果表明诱导了细胞凋亡。这种使用雷帕霉素的药物递送系统可能是治疗乳腺癌的潜在候选方案。
