Glioma is one of the most common primary intracranial tumor, but the current treatments of glioma are far from satisfying. As the major treatment option for malignant glioma, chemotherapy has its own disadvantages, including low chemotherapeutic agents delivery across blood-brain barrier (BBB) and lack of specificity. Therefore, new approach permitting glioma targeting ability that can allow an efficient therapeutic delivery into the glioma regions is urgently required. Ligand-mediated liposomes have shown great potential for improving the efficiency of glioma treatment. In our study, the multi-targeting liposomes based on glucose and biotin were constructed for the first time. We synthesized two ligands (Glu₃-Chol, Bio₂-Chol), prepared three types of modified liposomes (Glu₃-Lip, Bio₂-Lip and Bio₂+Glu₃-Lip) and evaluated the glioma-targeting ability of these liposomes which were using paclitaxel (PTX) as the model drug in vitro. Besides, the uptake mechanism of Bio₂+Glu₃-Lip was investigated. PTX-loaded Bio₂+Glu₃-Lip (PTX-Bio₂+Glu₃-Lip) exhibited satisfactory targeting effect in Bend.3 and C6 cells in vitro, in which the cellular uptake of Bio₂+Glu₃-Lip were 4.04- and 3.49-fold more than that of the uncoated liposomes (Lip). The results suggested the multi-targeting liposomes (Bio₂+Glu₃-Lip) is a promising formulation for glioma, which was almost consistent with the results of in vivo imaging. In summary, we have designed and fabricated an effective delivery system to treat glioma.

胶质瘤是最常见的原发性颅内肿瘤之一，但目前对胶质瘤的治疗还远远不能令人满意。作为恶性胶质瘤的主要治疗选择，化疗有其自身的缺点，包括跨血脑屏障 (BBB) 的低化疗药物递送和缺乏特异性。因此，迫切需要一种允许神经胶质瘤靶向能力的新方法，该方法可以有效地将治疗递送到神经胶质瘤区域。配体介导的脂质体已显示出提高胶质瘤治疗效率的巨大潜力。在我们的研究中，首次构建了基于葡萄糖和生物素的多靶向脂质体。我们合成了两种配体（Glu ₃ -Chol、Bio ₂ -Chol），制备了三种类型的修饰脂质体（Glu₃ -Lip、Bio ₂ -Lip 和 Bio ₂ +Glu ₃ -Lip)，并在体外评估了这些使用紫杉醇 (PTX) 作为模型药物的脂质体的胶质瘤靶向能力。此外，还研究了Bio ₂ +Glu ₃ -Lip的吸收机制。PTX-loaded Bio ₂ +Glu ₃ -Lip (PTX-Bio ₂ +Glu ₃ -Lip) 在体外Bend.3和C6细胞中表现出令人满意的靶向效果，其中Bio ₂ +Glu ₃ -Lip的细胞摄取率为4.04 - 比未包被的脂质体 (Lip) 高 3.49 倍。结果表明多靶向脂质体（Bio ₂ +Glu_3- Lip) 是一种很有前景的胶质瘤制剂，这与体内成像的结果几乎一致。总之，我们设计并制造了一种有效的递送系统来治疗神经胶质瘤。