Membrane-disruptive peptides/peptidomimetics (MDPs) are antimicrobials or anticarcinogens that present a general killing mechanism through the physical disruption of cell membranes, in contrast to conventional chemotherapeutic drugs, which act on precise targets such as DNA or specific enzymes. Owing to their rapid action, broad-spectrum activity, and mechanisms of action that potentially hinder the development of resistance, MDPs have been increasingly considered as future therapeutics in the drug-resistant era. Recently, growing experimental evidence has demonstrated that MDPs can also be utilized as adjuvants to enhance the therapeutic effects of other agents. In this review, we evaluate the literature around the broad-spectrum antimicrobial properties and anticancer activity of MDPs, and summarize the current development and mechanisms of MDPs alone or in combination with other agents. Notably, this review highlights recent advances in the design of various MDP-based drug delivery systems that can improve the therapeutic effect of MDPs, minimize side effects, and promote the co-delivery of multiple chemotherapeutics, for more efficient antimicrobial and anticancer therapy.

膜破坏肽/肽模拟物 (MDP) 是抗微生物剂或抗癌剂，与传统的化疗药物相反，它们通过细胞膜的物理破坏呈现出一般的杀伤机制，后者作用于 DNA 或特定酶等精确目标。由于其快速作用、广谱活性和可能阻碍耐药性发展的作用机制，MDPs 越来越多地被认为是耐药时代的未来疗法。最近，越来越多的实验证据表明，MDPs 也可以用作佐剂来增强其他药物的治疗效果。在这篇综述中，我们评估了关于 MDP 的广谱抗菌特性和抗癌活性的文献，并总结 MDPs 单独或与其他药物联合使用的当前发展和机制。值得注意的是，这篇综述强调了各种基于 MDP 的药物递送系统设计的最新进展，这些系统可以提高 MDP 的治疗效果，最大限度地减少副作用，并促进多种化疗药物的共同递送，以实现更有效的抗菌和抗癌治疗。