Water-soluble supramolecular polymers can be created by incorporation of self-complementary multiple hydrogen bonding groups. However, technically simple fabrication of water-soluble supramolecular polymers with highly desirable physical properties—to achieve micelles suitable for effective delivery of drugs for cancer treatment—remains a significant challenge. We developed a new polyethylene glycol-based supramolecular polymer containing self-complementary quadruple hydrogen bonding groups, which spontaneously assembles into nanospherical micelles in an aqueous environment. These supramolecular micelles can be readily controlled to obtain the desired structural stability and possess excellent pH-responsive and drug-loading capabilities, as well as good biocompatibility towards both normal and cancer cells. The resulting drug-loaded micelles exhibit tunable drug loading capacity and excellent long-term drug-entrapment stability due to the strong affinity between the drug and micelle core, which led to highly efficient drug loading. In addition, in vitro release assays indicated the drug-loaded micelles can be triggered to rapidly release the drug under mildly acidic conditions. More importantly, fluorescence microscopy and flow cytometry clearly demonstrated that drug-loaded micelles were effectively endocytosed by cancer cells and induced apoptosis; therefore, this newly developed supramolecular system could serve as versatile drug nanovehicle for safe, effective controlled drug release to achieve superior chemotherapeutic effects.

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氢键超分子胶束介导的药物递送增强了癌症化学疗法的效力和安全性

水溶性超分子聚合物可以通过结合自我互补的多个氢键基团来产生。然而，具有高度期望的物理性质的水溶性超分子聚合物的技术简单制造（以实现适于有效递送用于癌症治疗的药物的胶束）仍然是一个重大挑战。我们开发了一种新的基于聚乙二醇的超分子聚合物，该聚合物包含自互补的四氢键合基团，该基团在水性环境中自发组装成纳米球形胶束。这些超分子胶束可以容易地控制以获得所需的结构稳定性，并具有出色的pH响应和载药能力，以及对正常细胞和癌细胞的良好生物相容性。由于药物与胶束核心之间的强亲和力，所得的载药胶束显示出可调节的载药量和出色的长期载药稳定性，从而导致高效载药。此外，体外释放试验表明，载有药物的胶束可以在弱酸性条件下迅速释放。更重要的是，荧光显微镜和流式细胞术清楚地表明载药的胶束被癌细胞有效地内吞并诱导了细胞凋亡。因此，这种新开发的超分子系统可作为通用的药物纳米载体，用于安全，有效地控制药物释放，以实现出色的化学治疗效果。