Glucocorticoids (GC) are common drugs used to treat acute and chronic inflammatory diseases, whose prolonged use can result in severe side effects hampering their efficacy. In addition, the pharmacokinetics, and biodistribution of GC are inadequate to support high efficacy with reduced toxicity. Following the marketing of GC prodrugs, new GC prodrug entities, and conjugates, have been developed. These new prodrugs and conjugates have been administered in free form or under a nanoparticulate form for local or systemic administration. These nanoparticles from lipid prodrugs and nanoconjugates change the paradigm of GC delivery, solving the issue of low drug loading into nanoparticles and circumventing the potential burst release effect by allowing a more controlled delivery of the GC and better targeting in inflammatory sites. This review highlights the design strategies, recent advances in GC prodrugs and conjugates, and their delivery in nanoparticulate form, demonstrating the strong potentialities of these novel strategies.

糖皮质激素 (GC) 是用于治疗急性和慢性炎症性疾病的常用药物，长期使用会导致严重的副作用，从而影响其疗效。此外，GC 的药代动力学和生物分布不足以支持高效和低毒性。随着 GC 前药的上市，已经开发了新的 GC 前药实体和缀合物。这些新的前药和偶联物以游离形式或纳米颗粒形式用于局部或全身给药。这些纳米粒子脂质前药和纳米偶联物改变了 GC 递送的范例，解决了纳米颗粒载药量低的问题，并通过允许更受控的 GC 递送和更好地靶向炎症部位来规避潜在的爆发释放效应。这篇综述重点介绍了设计策略、GC 前药和偶联物的最新进展，以及它们以纳米颗粒形式的递送，展示了这些新策略的强大潜力。