Department of Organic Chemistry Center for Research in Biological Chemistry & Molecular Materials (CIQUS), University of Santiago de Compostela, Jenaro de la Fuente s/n, 15782, Santiago de Compostela, Spain.
Pharm Res. 2012 Apr;29(4):902-21. doi: 10.1007/s11095-012-0683-y. Epub 2012 Jan 25.
During the last decades, great efforts have been devoted to design polymers for reducing the toxicity, increasing the absorption, and improving the release profile of drugs. Advantage has been also taken from the inherent multivalency of polymers and dendrimers for the incorporation of diverse functional molecules of interest in targeting and diagnosis. In addition, polymeric hydrogels with the ability to encapsulate drugs and cells have been developed for drug delivery and tissue engineering applications. In the long road to this successful story, pharmaceutical sciences have been accompanied by parallel advances in synthetic methodologies allowing the preparation of precise polymeric materials with enhanced properties. In this context, the introduction of the click concept by Sharpless and coworkers in 2001 focusing the attention on modularity and orthogonality has greatly benefited polymer synthesis, an area where reaction efficiency and product purity are significantly challenged. The purpose of this Expert Review is to discuss the impact of click chemistry in the preparation and functionalization of polymers, dendrimers, and hydrogels of interest in drug delivery.
在过去的几十年中,人们致力于设计聚合物以降低药物毒性、增加药物吸收并改善药物释放特性。人们还充分利用聚合物和树枝状大分子固有的多价性,将不同的功能分子整合到靶向和诊断中。此外,还开发了具有封装药物和细胞能力的聚合物水凝胶,用于药物输送和组织工程应用。在这个成功故事的漫长道路上,制药科学伴随着合成方法的平行发展,这些方法可以制备具有增强性能的精确聚合物材料。在这种情况下,Sharpless 及其同事在 2001 年引入的点击概念将注意力集中在模块化和正交性上,这极大地促进了聚合物合成,在该领域,反应效率和产物纯度受到了极大的挑战。本文的目的是讨论点击化学在药物输送中感兴趣的聚合物、树枝状大分子和水凝胶的制备和功能化中的作用。