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制备、表征及评价载依托泊苷的聚乙二醇化纳米脂质体在肺癌中的作用。

Preparation, characterization and evaluation of PEGylated nanoliposomal containing etoposide on lung cancer.

机构信息

a Department of Chemical Engineering, Science and Research Branch, Islamic Azad University , Tehran , Iran.

b Department of Pilot Nanobiotechnology, Pasteur Institute of Iran , Tehran , Iran.

出版信息

Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):3222-3230. doi: 10.1080/21691401.2019.1646265.

Abstract

Lung cancer is the most common one in terms of outbreak and mortality. Since most modern treatments have many side effects, finding an effective and alternative therapy seems necessary. The present study aimed to determine the effect of PEGylated liposomal etoposide nanoparticles on the lung cancer (A-549 and Calu6 cell lines). The PEGylated liposomal etoposide nanoparticles were prepared by reverse-phase evaporation method. The particle size and zeta potential of the nanoparticles were measured by Zetasizer. The nanoparticle cytotoxicity was examined by MTT method. The vesicular drug release pattern was examined by dialysis method. The amount of loaded drug and the encapsulation efficiency (EE) was also measured and calculated. Apoptosis test was performed using flow cytometry with Annexin V kit. The mean particle size, size distribution, and zeta potential of PEGylated liposomal etoposide nanoparticles were 122.5 ± 4.8 nm, 0.252 ± 0.12 and -13.7 ± 0.51 mv, respectively. The etoposide release in prepared formulations was detected to be about 15.64% after 50 hr. The cytotoxic effect of etoposide nanoparticles on lung cancer A-549 and Calu6 cell lines showed more anti-tumour activity compared to the free drug used. The results showed that the PEGylated liposomal nanoparticles were used as a suitable nanocarrier for etoposide injection. It was also found that the drug effect on the nanodrug formulations was higher than that of the free drug.

摘要

肺癌在发病率和死亡率方面最为常见。由于大多数现代治疗方法有许多副作用,因此寻找一种有效且替代的治疗方法似乎是必要的。本研究旨在确定聚乙二醇化脂质体依托泊苷纳米粒对肺癌(A-549 和 Calu6 细胞系)的影响。聚乙二醇化脂质体依托泊苷纳米粒采用反相蒸发法制备。采用 Zetasizer 测量纳米粒的粒径和zeta 电位。采用 MTT 法检测纳米粒的细胞毒性。采用透析法检测囊泡药物释放模式。还测量并计算了载药量和包封效率(EE)。采用 Annexin V 试剂盒通过流式细胞术进行凋亡试验。聚乙二醇化脂质体依托泊苷纳米粒的平均粒径、粒径分布和 zeta 电位分别为 122.5±4.8nm、0.252±0.12 和-13.7±0.51mv。在 50 小时后,检测到制备的制剂中依托泊苷的释放量约为 15.64%。与使用的游离药物相比,依托泊苷纳米粒对肺癌 A-549 和 Calu6 细胞系的细胞毒性作用显示出更强的抗肿瘤活性。结果表明,聚乙二醇化脂质体纳米粒可用作依托泊苷注射液的合适纳米载体。还发现纳米药物制剂的药物作用高于游离药物。

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