Low-Density Lipoprotein-Mimicking Nanoparticles for Tumor-Targeted Theranostic Applications
Low-Density Lipoprotein-Mimicking Nanoparticles for Tumor-Targeted Theranostic Applications
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DOI：
10.1002/smll.201303277
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发表时间：
2015-01-14
期刊：
影响因子：
13.3
通讯作者：
Nam, Yoon Sung
中科院分区：
文献类型：
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作者：
Lee, Jeong Yu;Kim, Jin-Ho;Nam, Yoon Sung
这项研究引入了多功能脂质纳米粒子（LNP），模仿低密度脂蛋白的结构和成分，用于抗癌药物和超顺磁性纳米晶体的肿瘤靶向共同递送。紫杉醇（4.7 wt%）和氧化铁纳米晶体（6.8 wt%，直径 11 nm）被共同封装在叶酸功能化的 LNP 中，其中包含总直径约为 170 nm 的纳米晶体簇，zeta 电位约为 -40 mV。叶酸功能化的 LNP 能够在 T-2 加权磁共振图像中靶向检测 MCF-7（表达叶酸受体的人乳腺癌），并实现紫杉醇的有效细胞内递送。不含紫杉醇的 LNP 在浓度高达 0.2 mg mL(-1) 时未表现出明显的细胞毒性，表明 LNP 在细胞内药物输送应用中具有出色的生物相容性。 LNP 在小鼠肿瘤模型中的靶向抗肿瘤活性表明，低密度脂蛋白模拟 LNP 可以成为一种有效的治疗诊断平台，具有良好的生物相容性，可用于肿瘤靶向共递送各种抗癌药物。
This study introduces multifunctional lipid nanoparticles (LNPs), mimicking the structure and compositions of low-density lipoproteins, for the tumor-targeted co-delivery of anti-cancer drugs and superparamagnetic nanocrystals. Paclitaxel (4.7 wt%) and iron oxide nanocrystals (6.8 wt%, 11 nm in diameter) are co-encapsulated within folate-functionalized LNPs, which contain a cluster of nanocrystals with an overall diameter of about 170 nm and a zeta potential of about -40 mV. The folate-functionalized LNPs enable the targeted detection of MCF-7, human breast adenocarcinoma expressing folate receptors, in T-2-weighted magnetic resonance images as well as the efficient intracellular delivery of paclitaxel. Paclitaxel-free LNPs show no significant cytotoxicity up to 0.2 mg mL(-1), indicating the excellent biocompatibility of the LNPs for intracellular drug delivery applications. The targeted anti-tumor activities of the LNPs in a mouse tumor model suggest that the low-density lipoprotein-mimetic LNPs can be an effective theranostic platform with excellent biocompatibility for the tumor-targeted co-delivery of various anti-cancer agents.