Hematology and Oncology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Immunology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Pharm Dev Technol. 2021 Nov;26(9):934-942. doi: 10.1080/10837450.2021.1963276. Epub 2021 Aug 25.
Acriflavine (ACF) is an antiseptic compound with the potential antitumor activity which is used for the fluorescent staining of RNA due to its dominant fluorescent emission at ∼515 nm. Here, solid lipid nanoparticles (SLNs) containing ACF (ACF-SLNs) were prepared and their physicochemical properties, potential geno/cytotoxicity, as well as the fluorescent properties were investigated. FITC-annexin V/PI staining and cell cycle assays were carried out to find the type of cellular death caused. Particle size analysis and SEM images revealed that spherical ACF-SLNs had a homogeneous dispersion with a mean diameter of 106 ± 5.7 nm. Drug loading (DL) of 31.25 ± 4.21 mg/mL and high encapsulation efficiency (EE%) (89.75 ± 5.44) were found. ACF-SLNs physically were relatively stable in terms of dispersion, size, and EE. The uptake study demonstrated the potential use of fluorescent ACF-SLNs in bio-distribution studies. MTT assay showed that plain ACF could induce growth inhibition of A549 cells with of 8.5, 6, and 4.5 after 24, 48, and 72 hours, respectively, while ACF-SLNs had stable cytotoxic effects after 48 hours. ACF-SLNs induced remarkable apoptosis and even necrosis after 48 h. Conclusively, ACF-SLNs with acceptable physicochemical features showed increased bioimpacts after 48 h compared to plain ACF.
吖啶黄素(ACF)是一种具有潜在抗肿瘤活性的防腐剂化合物,由于其在 ∼515nm 处的主导荧光发射,因此被用于 RNA 的荧光染色。在这里,制备了含有吖啶黄素的固体脂质纳米粒(ACF-SLNs),并研究了它们的理化性质、潜在的遗传毒性/细胞毒性以及荧光特性。通过 FITC-annexin V/PI 染色和细胞周期分析来确定引起的细胞死亡类型。粒径分析和 SEM 图像表明,球形 ACF-SLNs 具有均匀的分散性,平均粒径为 106±5.7nm。发现药物载量(DL)为 31.25±4.21mg/mL,包封效率(EE%)高(89.75±5.44)。ACF-SLNs 在分散性、粒径和 EE 方面相对稳定。摄取研究表明,荧光 ACF-SLNs 具有在生物分布研究中潜在的应用价值。MTT 测定表明,普通 ACF 在 24、48 和 72 小时后分别对 A549 细胞的生长抑制率为 8.5、6 和 4.5,而 ACF-SLNs 在 48 小时后具有稳定的细胞毒性作用。ACF-SLNs 在 48 小时后诱导明显的凋亡,甚至坏死。总之,与普通 ACF 相比,具有可接受的理化特性的 ACF-SLNs 在 48 小时后表现出更大的生物影响。