Chemodrugs have been widely used to treat cancer; however, the chemotherapy usually leads to serious side effects and failure. Various nanomaterials and strategies have been explored for drug delivery to improve the efficacy of chemodrugs. One key to loading chemodrugs onto a nano-delivery system is enhancement of the encapsulation efficiency, especially for polymeric nanoparticles being loaded with hydrophilic drugs. Inspired by the ability of eukaryote to package millions of genes in the nucleus wrapping and condensing DNA around histones to form chromosomes, here we developed a karyon-like hybrid nanoparticle to achieve ultra-high encapsulation of doxorubicin (Dox) with reduced side effects. We utilized fullerenol as a “histone”, packaged a great number of Dox, and used PEG-PLGA as the “karyotheca” coating the “nucleosome” (fullerenol and Dox complex) to stabilize the complex. It is noteworthy that the encapsulation efficiency of Dox in the polymeric micelles was increased from ∼5% to ∼79%. What's more, the biomimetic-inspired delivery system significantly reduced the chemodrug side effects by utilizing the radical scavenging ability of fullerenol. This novel drug-delivery design approach provides useful insights for improving the applicability of fullerenol in other drug delivery systems for cancer therapy.

化学药品已被广泛用于治疗癌症。然而，化学疗法通常导致严重的副作用和失败。已经探索了用于药物递送的各种纳米材料和策略，以改善化学药品的功效。将化学药物装载到纳米递送系统上的一个关键是提高包封效率，尤其是对于装载了亲水性药物的聚合物纳米颗粒而言。受到真核生物将数百万个基因包装在细胞核中并围绕组蛋白浓缩DNA以形成染色体的能力的启发，我们在此开发了一种核样混合纳米颗粒，以实现阿霉素（Dox）的超高包封且具有减少的副作用。我们将富勒烯醇用作“组蛋白”，包装了许多Dox，并使用PEG-PLGA作为“核仁”，包被“核小体”（富勒烯醇和Dox复合物）以稳定复合物。值得注意的是，聚合物胶束中Dox的包封效率从5％增至79％。更重要的是，仿生启发式递送系统通过利用富勒烯醇的自由基清除能力，大大降低了化学药物的副作用。这种新颖的药物递送设计方法为改善富勒烯醇在其他用于癌症治疗的药物递送系统中的适用性提供了有用的见识。仿生启发的递送系统通过利用富勒烯醇的自由基清除能力，大大降低了化学药物的副作用。这种新颖的药物递送设计方法为改善富勒烯醇在其他用于癌症治疗的药物递送系统中的适用性提供了有用的见识。仿生启发的递送系统通过利用富勒烯醇的自由基清除能力，大大降低了化学药物的副作用。这种新颖的药物递送设计方法为改善富勒烯醇在其他用于癌症治疗的药物递送系统中的适用性提供了有用的见识。