Nano-sized cationic polymeric magnetic liposomes significantly improves drug delivery to the brain in rats
Nano-sized cationic polymeric magnetic liposomes significantly improves drug delivery to the brain in rats
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DOI：
10.3109/1061186x.2011.651726
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发表时间：
2012-06-01
影响因子：
4.5
通讯作者：
Li, Anmin
中科院分区：
文献类型：
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作者：
Zhao, Ming;Chang, Jin;Li, Anmin
近年来，阳离子聚合物磁性脂质体比传统脂质体表现出更高的稳定性和更长的循环半衰期。在这里，我们检查了阳离子聚合物磁性脂质体在以紫杉醇为负载剂的磁性靶向下将药物递送至大脑的能力。我们发现制备的负载紫杉醇的磁性脂质体具有20 nm的均匀直径并且具有超顺磁性。通过尾静脉注射到大鼠体内后，未磁靶向时脑内紫杉醇浓度增加了2-5倍，磁靶向后脑内紫杉醇浓度增加了5-15倍。高脑浓度维持时间超过8 h，明显长于纯紫杉醇注射液。当通过颈内动脉给予脂质体的剂量为尾静脉给药剂量的10%时，脑内紫杉醇增加了1.5倍，表明动脉内给药显着提高了递送效率。皮层的普鲁士蓝染色显示，磁性脂质体聚集在皮层脉管系统中，并且皮层细胞处于磁性靶向之下，这表明药物被递送穿过几乎不可渗透的血脑屏障。这些结果表明，纳米尺寸的阳离子聚合物磁性脂质体是磁性药物递送至大脑的潜在工具。
In recent years, cationic polymeric magnetic liposomes have shown greater stability and prolonged circulation half-life over traditional liposomes. Here, we examined the capability of cationic polymeric magnetic liposomes in delivering drugs into the brain under magnetic targeting with paclitaxel as the loaded agent. We found that the fabricated paclitaxel-loaded magnetic liposomes had a uniform diameter of 20 nm and were superparamagnetic. After they were injected into rats by the caudal vein, brain paclitaxel concentration increased 2-5 folds without magnetic targeting and 5-15 folds after magnetic targeting. The high brain concentration was maintained for more than 8 h, which was significantly longer than that for pure paclitaxel injection. When the liposomes were given via the internal carotid artery at 10% of the dose given via the caudal vein, paclitaxel in the brain was increased by 1.5 folds, indicating that intra-arterial administration enhanced delivery efficiency remarkably. Prussian blue staining of the cortex showed that the magnetic liposomes were aggregated in the cortex vasculature and the cortex cells were under magnetic targeting, indicating that the drugs were delivered across the nearly impermeable blood-brain barrier. These results showed that the nano-sized cationic polymeric magnetic liposomes are potential tools for magnetic drug delivery to the brain.