Enhanced cytocompatibility and functional group content of poly( l -lysine) dendrimers by grafting with poly(oxazolines)
Enhanced cytocompatibility and functional group content of poly( l -lysine) dendrimers by grafting with poly(oxazolines)
复制标题
通过接枝聚恶唑啉增强聚（L-赖氨酸）树枝状聚合物的细胞相容性和官能团含量
DOI：
10.1039/c6py00478d
复制
发表时间：
2016
影响因子：
4.6
通讯作者：
England R
中科院分区：
文献类型：
--
作者：
England R
当考虑先进药物递送系统的设计时，常见的期望属性是在血液循环中具有延长的停留时间，使得在感兴趣的部位（例如肿瘤）处可以发生积聚和局部有效负载释放。聚乙二醇（PEG）一直是满足这一要求的金标准，因此已被充分研究作为材料的表面改性的树枝状聚合物。作为替代方案，我们已经探索了使用聚恶唑啉（POZ）作为用于修饰第5代L-赖氨酸树枝状聚合物表面的材料，并发现与未修饰的树枝状聚合物相比，生物相容性有显著改善。POZ相对于PEG的一个特别有用的优点在于我们能够利用其赋予功能性的主链侧基。修改POZ有悬垂羧基导致一种新的改性树枝状大分子具有显着更多的共轭位点。由此，我们证明，与无功能的POZ等效物相比，香豆素（我们的模型化合物）的载量增加了六倍。
When considering the design of an advanced drug delivery system, a common desirable attribute is to have a prolonged residence time in blood circulation so that accumulation and localised payload release may occur at the site of interest (e.g. a tumour). Polyethylene glycol (PEG) has been a gold standard for fulfilling this requirement, and consequently has been well investigated as a material for surface modification of dendrimers. As an alternative, we have explored the use of polyoxazolines (POZ)s as materials for modifying the surface of a generation 5 L-lysine dendrimer and found that there was a significant improvement in the biocompatibility properties over the unmodified dendrimer. One particularly useful advantage of POZ over PEG lies in the main-chain pendant groups available that we were able to exploit to impart functionality. Modifying the POZ to have pendant carboxyl groups led to a novel modified dendrimer with significantly more sites for conjugation. With this, we have demonstrated a sixfold increase in the loading of coumarin (our model compound) when compared to a non-functional POZ equivalent.