A Passerini three-component polymerization was performed for the synthesis of amphiphilic star-shaped block copolymers with hydrophobic cores and hydrophilic coronae. The degree of polymerization of the hydrophobic core was varied from 5 to 10 repeating units, and the side chain ends were conjugated by performing a Passerini-3CR with PEG-isocyanide and PEG-aldehyde (950 g/mol). The resulting amphiphilic star-shaped block copolymers contained thioether groups, which could be oxidized to sulfones in order to further tune the polarity of the polymer chains. The ability of the amphiphilic copolymers to act as unimolecular micellar encapsulants was tested with the water-insoluble dye Orange II, the water-soluble dye Para Red and the macrolide antibiotic azithromycin. The results showed that the new copolymers were able to retain drug cargo at pH levels corresponding to circulating blood and selectively release therapeutically effective doses of antibiotic as measured by bacterial cell kill. The polymers were also well-tolerated by differentiated THP-1 macrophages in the absence of encapsulated drugs.

中文翻译：

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通过Passerini反应获得的生物相容性单分子胶束，作为多功能纳米载体，可用于潜在的医学应用。

进行Passerini三组分聚合反应，以合成具有疏水核和亲水冠的两亲星形嵌段共聚物。疏水核的聚合度在5到10个重复单元之间变化，并且侧链末端通过用PEG-异氰化物和PEG-醛（950 g / mol）进行Passerini-3CR进行缀合。所得的两亲星形嵌段共聚物包含硫醚基团，可以将其氧化为砜，以进一步调节聚合物链的极性。用水不溶性染料Orange II，水溶性染料对红和大环内酯类抗生素阿奇霉素测试了两亲共聚物充当单分子胶束密封剂的能力。结果表明，新的共聚物能够在与循环血液相对应的pH值水平下保留药物负载，并选择性释放治疗有效剂量的抗生素（通过细菌细胞杀伤法测定）。在没有包封药物的情况下，分化的THP-1巨噬细胞对聚合物的耐受性也很好。