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Transferrin and folic acid co-modified bufalin-loaded nanoliposomes: preparation, characterization, and application in anti-cancer activity

机译:转铁蛋白和叶酸共修饰的蟾蜍灵负载纳米脂质体:制备,表征和在抗癌活性中的应用

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Aim: The aim of this study was to prepare transferrin (Tf) and folic acid (FA) co-modified bufalin (BF) liposomes for lung cancer treatment. Method: In this study, (FA+Tf) BF-LPs were prepared using the high-pressure homogenization method. Results: The EE% and DL% of prepared LPs were 82.3% and 10.7%, respectively, and the mean diameter was 120.4 nm from three batches. In vitro release showed that the release of BF from (FA+Tf) BF-LPs was slow with burst effects at an early stage. In vitro cytotoxicity assay showed that (FA+Tf) BF-LPs had a superior antiproliferative effect on A549 cells. An in vivo imaging study indicated that (FA+Tf) BF-LPs had obvious targeting characteristics on subcutaneous tumor, with the potential to actively deliver drugs to tumor tissues. In terms of the in?vivo antitumor activity, (FA+Tf) BF-LPs treated mice showed a significantly suppressed tumor growth and no systemic toxicity in the body. Conclusion: Through this study, it was found that the Tf and FA co-modified BF could be a very promising lung target preparation.
机译:目的:本研究的目的是制备转铁蛋白(Tf)和叶酸(FA)共修饰的蟾蜍灵(BF)脂质体,以治疗肺癌。方法:在本研究中,使用高压均质方法制备了(FA + Tf)高炉-LP。结果:制备的LP的EE%和DL%分别为82.3%和10.7%,三个批次的平均直径为120.4 nm。体外释放表明,从(FA + Tf)BF-LPs中释放BF较慢,在早期具有爆发效应。体外细胞毒性试验表明,(FA + Tf)BF-LPs对A549细胞具有优异的抗增殖作用。体内成像研究表明(FA + Tf)BF-LPs对皮下肿瘤具有明显的靶向特征,具有将药物主动递送至肿瘤组织的潜力。就体内抗肿瘤活性而言,经(FA + Tf)BF-LPs处理的小鼠显示出显着抑制的肿瘤生长,并且在体内没有全身毒性。结论:通过这项研究,发现Tf和FA共修饰的BF可能是非常有希望的肺靶标制剂。

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