Abstract Novel dendritic antibacterial copolymer (PCL20-KG5) mimicking antimicrobial peptide features is synthesized by using Polycaprolactone (PCL) and BOC-Lysine(BOC)-OSu. PCL20-NH2 is designed as the core, and BOC-lysine(BOC)-OSu reacts with amino groups generation by generation to form dendritic structures. The properties and morphologies of PCL20-KG5 and their assemblies are characterized via the plate counting method, hemolytic analysis, transmission electron microscopy, dynamic light scattering, and drug release experiment. Results showed that PCL20-KG5 has excellent broad-spectrum antibacterial activity and extremely low hemolytic toxicity. It achieves antibacterial effect via membrane destruction without inducement of drug resistance. In addition, PCL20-KG5 dendrimer copolymer can self-assemble into uniform stable vesicles. Drug release experiments showed that the vesicles possess efficient drug loading capacity and are beneficial to realize continuous drug release in clinical treatment.

中文翻译：

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聚己内酯-赖氨酸-树枝状聚合物组装制备的生物相容性抗菌纳米颗粒

摘要 采用聚己内酯（PCL）和BOC-赖氨酸（BOC）-OSu合成了具有抗菌肽特性的新型树枝状抗菌共聚物（PCL20-KG5）。以PCL20-NH2为核心设计，BOC-赖氨酸(BOC)-OSu与氨基代代反应形成树枝状结构。通过平板计数法、溶血分析、透射电子显微镜、动态光散射和药物释放实验表征了 PCL20-KG5 及其组件的性质和形态。结果表明PCL20-KG5具有优良的广谱抗菌活性和极低的溶血毒性。它通过破坏膜达到抗菌作用，不会引起耐药性。此外，PCL20-KG5 树枝状聚合物可以自组装成均匀稳定的囊泡。