Effect of PEG conformation and particle size on the cellular uptake efficiency of nanoparticles with the HepG2 cells
Effect of PEG conformation and particle size on the cellular uptake efficiency of nanoparticles with the HepG2 cells
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PEG构象和粒径对HepG2细胞纳米粒子细胞摄取效率的影响
DOI：
10.1016/j.jconrel.2006.11.028
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发表时间：
2007-03-12
影响因子：
10.8
通讯作者：
Wang, Chi-Hwa
中科院分区：
文献类型：
--
作者：
Hu, Yong;Xie, Jingwei;Wang, Chi-Hwa
聚己内酯（MePEG-PCL）和聚己内酯-聚（乙二醇）-聚己内酯的三嵌段共聚物（PCL-PEG-PCL）。MePEG-PCL共聚物在其表面上形成具有PEG“刷”的纳米颗粒，并且PCL-PEG-PCL共聚物在水溶液中在其表面上形成具有“蘑菇状”结构的纳米颗粒。采用场发射扫描电子显微镜（FESEM）和激光光散射（LLS）对纳米粒子的形貌和尺寸进行了表征。所有纳米粒子均为球形，粒径小于200 nm。纳米颗粒的尺寸随着PCL链段长度的增加而增加。载药量测定结果表明，紫杉醇与共聚物的最佳投料比取决于共聚物的组成，投料比以5%为宜。聚合物的体外释放行为表现为持续释放，并受聚合物组成的影响。实验结果表明，细胞更倾向于附着在疏水性更强的聚合物上。与疏水性相近的MePEG-PCL和PCL-PEG-PCL相比，由于PCL-PEG-PCL共聚物表面形成了更致密的PEG层，因此更多的HepG 2细胞附着在MePEG-PCL共聚物膜上。体外细胞摄取实验结果表明，HepG 2细胞更喜欢在其表面上具有相同PEG构型的较小纳米颗粒。紫杉醇纳米粒的细胞毒性似乎随着纳米粒对HepG 2细胞载药量的增加而增加。(c)2006年爱思唯尔B.V保留所有战斗。
polycaprolactone (MePEG-PCL) and triblock copolymer of polycaprolactone-poly(ethylene glycol)-polycaprolactone (PCL-PEG-PCL). The MePEG-PCL copolymers form nanoparticles with PEG "brush" on their surfaces and PCL-PEG-PCL copolymers form nanoparticles with a "mushroom-like" structure on their surfaces in aqueous solution. The morphology and size of nanoparticles were measured by field emission scanning electron microscopy (FESEM) and laser light scattering (LLS). All the nanoparticles are in spherical shape and the sizes are less than 200 nm. The sizes of the nanoparticles increases with increasing PCL segment length. The drug-loading content results showed that the optimal feeding ratio of paclitaxel to copolymer is dependent upon the copolymer composition and 5% is a suitable feeding ratio. The in vitro release behavior exhibits a sustained release manner and is affected by copolymer composition. Experimental results showed that cells would prefer to attach to more hydrophobic polymers. Comparing between MePEG-PCL and PCL-PEG-PCL of similar hydrophobicity, more HepG2 cells have attached to the MePEG-PCL copolymer films because a denser PEG layer was formed on the surfaces of PCL-PEG-PCL copolymers. In vitro cellular uptake experimental results indicated that HepG2 cells prefer smaller nanoparticles with the same PEG configuration on their surfaces. The cytotoxicity of paclitaxel-loaded nanoparticles seemed to increase with increasing drug loading of nanoparticles against HepG2 cells. (c) 2006 Elsevier B.V All fights reserved.