School of Nano Sciences, Central University of Gujarat, Gandhinagar, 382030, Gujarat, India.
School of Life Sciences, Central University of Gujarat, Gandhinagar, 382030, Gujarat, India.
Chem Phys Lipids. 2020 Nov;233:104978. doi: 10.1016/j.chemphyslip.2020.104978. Epub 2020 Sep 28.
Lung cancer is one of the most common malignant tumors and emerged as one of the leading causes of cancer-related death worldwide. Surgical resection can be a curative treatment for early stage but the most of lung cancer patients are diagnosed at an advanced stage when the pulmonary tumor has been invaded beyond the respiratory system. Therefore, chemotherapy is suitable for curing metastasized tumor. Baicalin (BL) is a flavonoid which has been studied in the treatment of several types of cancer including lung cancer. However, its low solubility in water and non-specificity impede its practical utilization. Hence, we have reported a stearic acid and pluronic F68 conjugated nanomicelles (PF68-SA) system to improve therapeutic efficacy of BL. Solvent evaporation method was used to prepare the BL-loaded PF68-SA nanomicelles (BLNM). The designed BLNM were characterized for the particle size, surface charge, critical micelle concentration, colloidal stability, morphology, and total drug content. BLNM formulation showed improved toxicity of BL against A549 human lung cancer cells in cytotoxicity assay. Further, apoptosis study also depicted BLNM-induced cell death in A549 cells. Therefore, the synthesized fatty acid-modified polymeric nanomicellar system could be useful in overcoming the stability and low therapeutic efficacy issues of hydrophobic anticancer drugs like BL and delivering them to the cancer cells.
肺癌是最常见的恶性肿瘤之一，也是全球癌症相关死亡的主要原因之一。手术切除可以作为早期阶段的一种治愈性治疗方法，但大多数肺癌患者在诊断时已经处于晚期，肺部肿瘤已经超出呼吸系统而发生了转移。因此，化疗适用于治疗转移性肿瘤。黄芩苷（BL）是一种黄酮类化合物，已被研究用于治疗多种类型的癌症，包括肺癌。然而，其在水中的溶解度低和非特异性阻碍了其实际应用。因此，我们报道了一种硬脂酸和聚氧乙烯醚 F68 共轭纳米胶束（PF68-SA）系统，以提高 BL 的治疗效果。采用溶剂蒸发法制备 BL 负载的 PF68-SA 纳米胶束（BLNM）。对设计的 BLNM 进行了粒径、表面电荷、临界胶束浓度、胶体稳定性、形态和总药物含量的表征。细胞毒性试验表明，BLNM 制剂提高了 BL 对人肺癌 A549 细胞的毒性。此外，凋亡研究也描绘了 BLNM 诱导 A549 细胞死亡。因此，合成的脂肪酸修饰的聚合物纳米胶束系统可以用于克服像 BL 这样的疏水性抗癌药物的稳定性和低治疗效果问题，并将它们递送到癌细胞中。
