These years, transformable drug delivery systems (DDSs), which hold the capability of changing formulation morphology and subsequent functionality at the desired disease site, have shown great promise in control of spatio-temporal drug delivery/release manner and enhanced treatment efficacy. Equipped with controllability and design flexibility, the transformable DDSs are being increasingly pursued for the development of precision drug delivery platforms for biomedical applications. In this review, we describe the recently developed intracelluarly and extracellularly transformable DDSs, especially associated with assembly or disassociation of the original formulation units, for achieving various functionalities, including prolonged retention time, inhibited endocytosis and enhanced cytotoxicity. Furthermore, the different stimuli, such as pH, enzyme, light, temperature, redox and mechanical force that trigger the transformation process are also introduced. The future outlook and challenges are discussed in the end.

近年来，可转换的药物输送系统（DDS）具有在所需疾病部位改变制剂形态和后续功能的能力，在控制时空药物输送/释放方式和增强治疗功效方面显示出了巨大的希望。具有可控制性和设计灵活性的可转换DDS越来越多地用于开发生物医学应用的精密药物输送平台。在这篇综述中，我们描述了最近开发的细胞内和细胞外可转化的DDS，特别是与原始配方单元的组装或解离有关的DDS，以实现各种功能，包括延长的保留时间，抑制内吞作用并增强细胞毒性。此外，还引入了引发转化过程的不同刺激，例如pH，酶，光，温度，氧化还原和机械力。最后讨论了未来的前景和挑战。