Emerging nanoparticle platforms to improve the administration of glucocorticoids

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.

Automated summary

Glucocorticoids (GC) are commonly used drugs for inflammatory diseases, but their prolonged use can lead to severe side effects. Recent advancements in GC prodrugs and conjugates, administered as free forms or nanoparticles, have improved drug delivery, controlled release, and targeting in inflammatory sites. This review highlights the potential of these novel strategies and discusses their design strategies and recent advances.