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载卡莫司汀的双离子固体脂质纳米粒表面抗表皮生长因子受体抑制人脑恶性神经胶质瘤细胞

Inhibition of human brain malignant glioblastoma cells using carmustine-loaded catanionic solid lipid nanoparticles with surface anti-epithelial growth factor receptor.

机构信息

Department of Chemical Engineering, National Chung Cheng University, Chia-Yi 62102, Taiwan, ROC.

出版信息

Biomaterials. 2011 Apr;32(12):3340-50. doi: 10.1016/j.biomaterials.2011.01.048. Epub 2011 Feb 5.

Abstract

Innovated catanionic solid lipid nanoparticles (CASLNs) carrying carmustine (BCNU) (BCNU-CASLNs) were grafted with anti-epithelial growth factor receptor (EGFR) (anti-EGFR/BCNU-CASLNs) and applied to inhibiting the propagation of human brain malignant glioblastomas cells. U87MG cells were treated with anti-EGFR/BCNU-CASLNs and stained for the expression of EGFR. The minimal average diameter of BCNU-CASLNs and maximal entrapment efficiency of BCNU emerged when the concentration of catanionic surfactants was 1 mm. An increase in the weight percentage of cacao butter (CB) reduced the zeta potential, enhanced the viability of human brain microvasscular endothelial cells (HBMECs), and decreased the expression of tumor necrosis factor-α by HBMECs. The dissolution rate of BCNU and inhibition against the multiplication of U87MG cells using anti-EGFR/BCNU-CASLNs followed the order: 100% CB > 0% CB > 50% CB. Anti-EGFR/BCNU-CASLNs demonstrated the properties including an effective delivery to U87MG cells and antiproliferative efficacy against the growth of malignant brain tumors.

摘要

载有卡莫司汀(BCNU)的创新型双阳离子固体脂质纳米粒(BCNU-CASLNs)与抗表皮生长因子受体(EGFR)(anti-EGFR/BCNU-CASLNs)接枝,并应用于抑制人恶性脑胶质瘤细胞的增殖。用抗 EGFR/BCNU-CASLNs 处理 U87MG 细胞并对 EGFR 的表达进行染色。当双阳离子表面活性剂的浓度为 1mm 时,BCNU-CASLNs 的最小平均直径和 BCNU 的最大包封效率出现。可可脂(CB)的重量百分比增加会降低 Zeta 电位,增强人脑微血管内皮细胞(HBMEC)的活力,并降低 HBMEC 中肿瘤坏死因子-α的表达。BCNU 的溶出率和用 anti-EGFR/BCNU-CASLNs 抑制 U87MG 细胞增殖的效果依次为:100% CB>0% CB>50% CB。Anti-EGFR/BCNU-CASLNs 表现出有效递送至 U87MG 细胞和抗增殖功效,可抑制恶性脑肿瘤的生长。

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