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Baicalin encapsulating lipid-surfactant conjugate based nanomicelles: Preparation, characterization and anticancer activity
Chemistry and Physics of Lipids ( IF 3.4 ) Pub Date : 2020-09-28 , DOI: 10.1016/j.chemphyslip.2020.104978
Ashok Kumar Jangid 1 , Hina Agraval 2 , Divya Bharti Rai 1 , Poonam Jain 1 , Umesh Cs Yadav 2 , Deep Pooja 3 , Hitesh Kulhari 1
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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.



中文翻译:

基于黄芩苷的脂质表面活性剂偶联物纳米胶束的制备、表征和抗癌活性

肺癌是最常见的恶性肿瘤之一,已成为全球癌症相关死亡的主要原因之一。手术切除可以是早期的治愈性治疗,但大多数肺癌患者在肺部肿瘤已侵入呼吸系统以外时被诊断为晚期。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,其在水中的低溶解度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普朗尼克 F68 共轭纳米胶束 (PF68-SA) 系统,以提高 BL 的治疗效果。溶剂蒸发法用于制备负载 BL 的 PF68-SA 纳米胶束 (BLNM)。对设计的 BLNM 进行粒度、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。BLNM 制剂在细胞毒性试验中显示 BL 对 A549 人肺癌细胞的毒性有所改善。此外,细胞凋亡研究还描述了 A549 细胞中 BLNM 诱导的细胞死亡。因此,合成的脂肪酸改性聚合物纳米胶束系统可用于克服疏水性抗癌药物如 BL 的稳定性和低疗效问题,并将其递送至癌细胞。细胞凋亡研究还描述了 A549 细胞中 BLNM 诱导的细胞死亡。因此,合成的脂肪酸改性聚合物纳米胶束系统可用于克服疏水性抗癌药物如 BL 的稳定性和低疗效问题,并将其递送至癌细胞。细胞凋亡研究还描述了 A549 细胞中 BLNM 诱导的细胞死亡。因此,合成的脂肪酸改性聚合物纳米胶束系统可用于克服疏水性抗癌药物如 BL 的稳定性和低疗效问题,并将其递送至癌细胞。

更新日期:2020-10-06
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