Abstract: Tacrolimus (TAC) is an immunosuppressant isolated from Streptomyces tsukubaensis that acts as a lipophilic immunosuppressant. It functions by inhibiting the production of interleukin-2 through the suppression of calcineurin activity and the blockade of IL-2 gene transcription, which ultimately attenuates T lymphocyte responses. Additionally, TAC impedes the release of inflammatory cytokines. These multifaceted mechanisms enable TAC to effectively manage conditions such as dry eye, spring keratoconjunctivitis, and corneal neovascularisation. Given its limited solubility in water (0.67±0.19) μg·mL⁻¹, TAC poses a challenge for formulation into conventional ophthalmic dosage forms. In an effort to surmount the solubility issue of TAC, recent years have witnessed the development of innovative ocular drug delivery systems for TAC. These delivery systems including liposomes, proglycosome nanovesicles, polymer micelles, nanoemulsions, nanoparticles, hydrogels, cyclodextrin inclusion compounds, and microcrystals, all of which are designed for the treatment of a range of ocular disorders and demonstrate considerable potential for application. The objective of this study is to critically review recent developments in the novel ocular formulations of TAC for the treatment of ocular diseases, thereby providing a comprehensive reference for future research and development in this field.