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Dendritic phospholipid-based drug delivery systems†
Biomaterials Science ( IF 5.8 ) Pub Date : 2018-01-16 00:00:00 , DOI: 10.1039/c7bm01001j
Lei Jiang 1, 2, 3, 4, 5 , Weizhi Chen 1, 2, 3, 4, 5 , Sensen Zhou 1, 2, 3, 4, 5 , Cheng Li 1, 2, 3, 4, 5 , Xiaoke Zhang 1, 2, 3, 4, 5 , Wei Wu 1, 2, 3, 4, 5 , Xiqun Jiang 1, 2, 3, 4, 5
Affiliation  

A class of new dendritic phospholipid compounds with different hydrophilic dendritic poly(L-lysine) peripheries from generations 1 (G1) to 3 (G3) (DPL-1 to DPL-3) were synthesised and nano-drug delivery systems based on these compounds were prepared (DPN-2 and DPN-3). DPL-1 couldn't self-assemble into nanocarriers. The size, TEM image, and the CD spectrum of DPN-2 and DPN-3 were experimentally examined. The effect of the peripheral structure of dendritic phospholipid-based nanocarriers on their biological performance and drug delivery efficiency was studied. In vitro cytotoxicity studies demonstrated that the DOX-loaded DPN-3 shows higher cytotoxicity against 4T1 cells and BGC823 cells than DPN-2. DOX-loaded DPN-3 also showed excellent behaviours in cell internalization and 4T1 multicellular spheroid penetration. The composition of the hydrophilic block in dendritic phospholipids affected the self-assembly behaviour, properties and delivery efficiency of the formed nanocarriers. This work will be helpful for building drug delivery systems with characteristics of high delivery efficiency and low cytotoxicity for clinical applications.

中文翻译:

基于树突磷脂的药物递送系统

合成了一类新的树突磷脂化合物,它们具有不同的亲水性树突状聚L-赖氨酸,从第1代(G1)到第3代(G3)(DPL-1到DPL-3),并且基于这些化合物的纳米药物递送系统准备(DPN-2和DPN-3)。DPL-1无法自组装为纳米载体。实验检测了DPN-2和DPN-3的大小,TEM图像和CD光谱。研究了树突状磷脂基纳米载体的外围结构对其生物学性能和药物递送效率的影响。体外细胞毒性研究表明,装载DOX的DPN-3对DT-2和BGC823细胞的杀伤力比DPN-2高。装载DOX的DPN-3在细胞内化和4T1多细胞球体渗透方面也表现出出色的行为。树突状磷脂中亲水性嵌段的组成影响所形成的纳米载体的自组装性能,性质和递送效率。这项工作将有助于为临床应用建立具有高递送效率和低细胞毒性特征的药物递送系统。
更新日期:2018-01-16
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