Amin Haitham, Osman Shaaban K, Mohammed Ahmed M, Zayed Gamal
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Al-Azhar University, Assiut 71524, Egypt.
Al-Azhar Centre of Nanosciences and Applications (ACNA), Al-Azhar University, Assiut 71524, Egypt.
Saudi Pharm J. 2023 Jan;31(1):29-54. doi: 10.1016/j.jsps.2022.11.004. Epub 2022 Nov 15.
Lung cancer is the number one killer among all cancer types. For decades, clinicians have been using conventional chemotherapeutics, but they can't rely on them alone anymore, because they poison bad cells and good cells as well. Researchers exploited nanotechnology as a potential tool to develop a platform for drug delivery to improve therapeutic efficiency. A quality by design synthesis of gefitinib-loaded starch nanoparticles (Gef-StNPs) has emerged as an essential tool to study and optimize the factors included in their synthesis. Therefore, we applied design of experiment (DOE) tools to attain the essential knowledge for the synthesis of high-quality Gef-StNPs that can deliver and concentrate the gefitinib (Gef) at A549 cells, thereby improving therapeutic efficacy and minimizing adverse effects. The cytotoxicity after exposing the A549 human lung cancer cells to the optimized Gef-StNPs was found to be much higher than that of the pure Gef (IC = 6.037 ± 0.24 and 21.65 ± 0.32 μg/mL, respectively). The optimized Gef-StNPs formula showed superiority over the pure Gef regarding the cellular uptake in A549 human cell line (3.976 ± 0.14 and 1.777 ± 0.1 μg/mL) and apoptotic population (77.14 ± 1.43 and 29.38 ± 1.11 %), respectively. The results elucidate why researchers have a voracious appetite for using natural biopolymers to combat lung cancer and paint an optimistic picture of their potential to be a promising tool in battling lung cancer.
肺癌是所有癌症类型中的头号杀手。几十年来，临床医生一直在使用传统化疗药物，但他们不能再仅仅依赖这些药物了，因为它们会同时毒害坏细胞和好细胞。研究人员利用纳米技术作为一种潜在工具来开发药物递送平台，以提高治疗效率。载有吉非替尼的淀粉纳米颗粒（Gef-StNPs）的质量源于设计合成已成为研究和优化其合成中所包含因素的重要工具。因此，我们应用实验设计（DOE）工具来获取合成高质量Gef-StNPs的基本知识，这种纳米颗粒能够在A549细胞中递送并浓缩吉非替尼（Gef），从而提高治疗效果并将副作用降至最低。将A549人肺癌细胞暴露于优化后的Gef-StNPs后发现，其细胞毒性远高于纯吉非替尼（IC分别为6.037±0.24和21.65±0.32μg/mL）。在A549人细胞系中的细胞摄取（分别为3.976±0.14和1.777±0.1μg/mL）和凋亡细胞群（分别为77.14±1.43和29.38±1.11%）方面，优化后的Gef-StNPs配方显示出优于纯吉非替尼的性能。这些结果阐明了为什么研究人员热衷于使用天然生物聚合物来对抗肺癌，并描绘了它们成为对抗肺癌的有前途工具的乐观前景。
