A synthetic strategy towards modular polymer platform capable of further tunable degree of modification is presented. Initially, a well-defined amphiphilic block copolymer with alkyne side groups distributed along the biodegradable hydrophobic block was successfully prepared applying controlled ring-opening copolymerization of D,L-lactide and an acetylene-functional cyclic carbonate initiated by polyoxyethylene macroinitiator. In the second synthetic step a desired number of cinnamyl pendant groups was introduced into the hydrophobic block via “click” reaction. The functional block copolymers self-associated in aqueous media into stable micelles with narrow size distribution and average diameters of around 50 nm. The micelles' functional hydrophobic cores were loaded with caffeic acid phenethyl ester (CAPE) as bioactive compound with great potential for therapeutic application. It was demonstrated that the initial drug-release profiles, hence the stability of the loaded nanocarriers during circulation, can be modulated via the number of cinnamyl groups into the micelles core. Initial in-vitro evaluations were preformed on empty and drug-loaded functional polymer micelles indicating their potential for application in nanomedicine as safe and biocompatible drug-delivery nanovehicles with enhanced stability.

提出了一种能够进一步调节修饰度的模块化聚合物平台的合成策略。最初，通过D，L-丙交酯与聚氧乙烯大分子引发剂引发的乙炔官能环状碳酸酯的受控开环共聚，成功制备了具有沿可生物降解的疏水嵌段分布的炔基侧基的定义明确的两亲嵌段共聚物。在第二个合成步骤中，将所需数量的肉桂基侧基通过“点击”反应。功能性嵌段共聚物在水性介质中自缔合成稳定的胶束，胶束的尺寸分布狭窄，平均直径约为50 nm。胶束的功能性疏水核负载有咖啡酸苯乙酯（CAPE）作为生物活性化合物，具有巨大的治疗应用潜力。已经证明，可以通过进入胶束核心的肉桂基基团的数量来调节初始药物释放曲线，从而可以调节循环过程中负载的纳米载体的稳定性。对空的和载有药物的功能聚合物胶束进行了初步的体外评估，表明它们在纳米药物中的应用潜力具有潜在的安全性和生物相容性，并且具有稳定的生物相容性纳米药物。