In this review we consider assembled nanodrugs as a type of nanoscale drugs formed by molecular self-assembly and associated with precise organization of multiple non-covalent interactions. Their typical feature is that the drug itself is considered as one of the building blocks with flexibly interplaying interaction for supramolecular assembly and nanostructure formation with robust stability and high loading efficiency in a controlled and tunable way. The super stability with retained function results from the “hydrophobic effect” of supramolecular self-assembly of peptides and drugs. It is the hydrophobic effect responsible for both colloidal stability and circulation stability in body against dilution and blood-flow shearing. The assembled nanodrugs are distinguished from conventional ones with encapsulation of the drugs in delivery nanocarriers. We will focus on how peptides and peptide-conjugates can be designed for controlling and mediating the formation of the assembled nanodrugs. Emphasis will be put on the rational design of intermolecular interactions between drugs and peptides, in vitro and in vivo drug delivery and antitumor therapeutic effects. Finally, we will discuss the key challenges and promising perspectives of such kind of peptide-mediated assembled nanodrugs for both technical advances and potential clinical translation.

在这篇综述中，我们认为组装的纳米药物是一种通过分子自组装形成的纳米级药物，与多种非共价相互作用的精确组织有关。它们的典型特征是，药物本身被认为是具有超分子组装和纳米结构形成的灵活相互作用的构建基块之一，具有可控和可调节的方式，具有强大的稳定性和高装载效率。具有保留功能的超稳定性是肽和药物的超分子自组装的“疏水作用”。它是疏水作用，既可以抵抗胶体稳定性，又可以抵抗稀释和血流切变，从而在体内的循环稳定性。组装好的纳米药物与常规的纳米药物的区别在于将药物封装在递送纳米载体中。我们将专注于如何设计肽和肽结合物来控制和介导组装的纳米药物的形成。重点将放在合理设计药物和肽之间的分子间相互作用，体外和体内药物递送以及抗肿瘤治疗效果上。最后，我们将讨论这种肽介导的组装纳米药物在技术进步和潜在临床翻译方面的主要挑战和有前途的观点。重点将放在合理设计药物和肽之间的分子间相互作用，体外和体内药物递送以及抗肿瘤治疗效果上。最后，我们将讨论这种肽介导的组装纳米药物在技术进步和潜在临床翻译方面的主要挑战和有前途的观点。重点将放在合理设计药物和肽之间的分子间相互作用，体外和体内药物递送以及抗肿瘤治疗效果上。最后，我们将讨论这种肽介导的组装纳米药物在技术进步和潜在临床翻译方面的主要挑战和有前途的观点。