Center for Education and Research on Macromolecules (CERM), University of Liege, B6 Sart-Tilman, B-4000 Liege, Belgium.
J Control Release. 2011 May 30;152(1):30-6. doi: 10.1016/j.jconrel.2011.03.026. Epub 2011 Mar 30.
Azido-functional amphiphilic macromolecules based on a biodegradable aliphatic polyester (poly-ε-caprolactone, PCL) and a bioeliminable hydrophilic poly(ethylene oxide) (PEO) block have been used in order to build micellar drug delivery systems. Such azido groups being able to react by alkyne-azide 1,3 Huisgens cycloaddition (a click reaction) have been used further in order to cross-link the micelles via redox-sensitive disulfide bridges. This reversible cross-linking allows to prevent micelle dissociation at high dilution upon injection and to trigger their dissociation in more reductive environment, such as the cytosol. Copolymers having three different architectures, i.e. able to cross-link either the core or the shell of core-shell-corona system have been used to investigate their micellization, cross-linking and cross-linking reversibility. The stealthiness of these micelles cross-linked in the hydrophobic segment has also been studied in vitro.
基于可生物降解脂肪族聚酯（聚己内酯，PCL）和可生物消除的亲水性聚（氧化乙烯）（PEO）嵌段的叠氮功能两亲性大分子已被用于构建胶束药物递送系统。这些叠氮基团能够通过炔烃-叠氮 1,3 Huisgens 环加成（点击反应）进行反应，进一步用于通过氧化还原敏感的二硫键交联胶束。这种可逆交联允许在注射时防止高稀释度下的胶束解离，并在更还原的环境（如细胞质）中触发它们的解离。使用具有三种不同结构的共聚物，即能够交联核壳核体系的核或壳，以研究其胶束化、交联和交联可逆性。还研究了这些在疏水区段交联的胶束的隐形性。
