Brain glioma is the most common primary tumour of the central nervous system. Complete surgical removal of the brain glioma is virtually impossible. Chemotherapy is still an important treatment for brain glioma. However, blood-brain barrier (BBB) and vasculogenic mimicry (VM) channels remain two hindrances in regular treatments. Herein, we developed a novel nanoscaled dual targeting daunorubicin plus rofecoxib liposomes which could transport across the BBB, and eliminate brain glioma cells along with the VM channels. The liposomes were modified with two functional materials, and showed round in shape with a diameter about 120 nm. Evaluations were performed on human brain glioma U87MG cells in vitro and on intracranial brain glioma-bearing nude mice. The dual targeting liposomes demonstrated a long circulatory effect in the blood system, were able to transport across the BBB, and were accumulated into the brain. The results indicated that the dual targeting daunorubicin plus rofecoxib liposomes could inhibit the brain glioma VM channels and exhibited a significant efficacy in the treatment of intracranial glioma-bearing nude mice. The mechanisms are related to down regulations MMP-2, MMP-9, FAK and HIF-α. Hence, the established dual targeting liposomes could be a potential formulation to treat the brain glioma along with eliminating VM channels.

中文翻译：

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纳米级双靶向载药脂质体抑制脑胶质瘤血管生成模拟通道的评价。

脑胶质瘤是中枢神经系统最常见的原发性肿瘤。完全手术切除脑胶质瘤几乎是不可能的。化疗仍然是脑胶质瘤的重要治疗方法。然而，血脑屏障 (BBB) 和血管生成拟态 (VM) 通道仍然是常规治疗的两个障碍。在此，我们开发了一种新型的纳米级双靶向柔红霉素加罗非昔布脂质体，可以跨 BBB 转运，并与 VM 通道一起消除脑胶质瘤细胞。脂质体经两种功能材料修饰，呈圆形，直径约120 nm。对体外人脑胶质瘤 U87MG 细胞和携带颅内脑胶质瘤的裸鼠进行了评估。双重靶向脂质体在血液系统中表现出长期的循环作用，能够穿过血脑屏障，并积累到大脑中。结果表明，双靶向柔红霉素联合罗非昔布脂质体可抑制脑胶质瘤VM通道，对颅内荷瘤裸鼠的治疗具有显着疗效。这些机制与下调 MMP-2、MMP-9、FAK 和 HIF-α 有关。因此，已建立的双靶向脂质体可能是治疗脑胶质瘤以及消除 VM 通道的潜在制剂。MMP-9、FAK 和 HIF-α。因此，已建立的双靶向脂质体可能是治疗脑胶质瘤以及消除 VM 通道的潜在制剂。MMP-9、FAK 和 HIF-α。因此，已建立的双靶向脂质体可能是治疗脑胶质瘤以及消除 VM 通道的潜在制剂。