Institute of Polymers, Bulgarian Academy of Sciences, Akad. G. Bonchev St., bl. 103-A, 1113 Sofia, Bulgaria.
Department of Biochemistry, Faculty of Biology, Sofia University "St. Kliment Ohridski", 8 Dragan Tzankov Blvd., 1164 Sofia, Bulgaria.
Int J Mol Sci. 2023 Jun 24;24(13):10588. doi: 10.3390/ijms241310588.
Polymer micelles represent one of the most attractive drug delivery systems due to their design flexibility based on a variety of macromolecular synthetic methods. The environmentally safe chemistry in which the use or generation of hazardous materials is minimized has an increasing impact on polymer-based drug delivery nanosystems. In this work, a solvent-free green synthetic procedure was applied for the preparation of an amphiphilic diblock copolymer consisting of biodegradable hydrophobic poly(acetylene-functional carbonate) and biocompatible hydrophilic polyethylene glycol (PEG) blocks. The cyclic functional carbonate monomer 5-methyl-5-propargyloxycarbonyl-1,3-dioxane-2-one (MPC) was polymerized in bulk using methoxy PEG-5K as a macroinitiator by applying the metal-free organocatalyzed controlled ring-opening polymerization at a relatively low temperature of 60 °C. The functional amphiphilic block copolymer self-associated in aqueous media into stable micelles with an average diameter of 44 nm. The copolymer micelles were physico-chemically characterized and loaded with the plant-derived anticancer drug curcumin. Preliminary in vitro evaluations indicate that the functional copolymer micelles are non-toxic and promising candidates for further investigation as nanocarriers for biomedical applications.
聚合物胶束因其基于各种高分子合成方法的设计灵活性而成为最具吸引力的药物传递系统之一。在环境安全化学中,尽量减少有害物质的使用或产生对基于聚合物的药物传递纳米系统有越来越大的影响。在这项工作中,采用无溶剂绿色合成工艺制备了由可生物降解的疏水性聚(乙炔基碳酸酯)和生物相容性的亲水性聚乙二醇(PEG)嵌段组成的两亲性嵌段共聚物。环状官能团碳酸酯单体 5-甲基-5-炔丙氧基羰基-1,3-二氧戊环-2-酮(MPC)在本体中使用甲氧基聚乙二醇 5K 作为大分子引发剂进行聚合,通过在相对较低的 60°C 温度下应用无金属有机催化的可控开环聚合进行聚合。功能两亲嵌段共聚物在水介质中自组装成平均直径为 44nm 的稳定胶束。对共聚物胶束进行了物理化学表征,并负载了植物来源的抗癌药物姜黄素。初步的体外评估表明,功能共聚物胶束是无毒的,有希望作为生物医学应用的纳米载体进一步研究。