Long-term clinical outcomes of 0.015 % tacrolimus HPβCD eye drops in ocular surface inflammatory disorders

Topical tacrolimus offers potent anti-inflammatory effects across a spectrum of ocular surface diseases, but its ophthalmic use has been limited by formulation challenges. This study evaluated 0.015 % tacrolimus/hydroxypropyl-β-cyclodextrin eye drops (TCD) long-term performance.

In a prospective, open-label, sequential design, 56 patients treated ≥6 months with 0.03 % tacrolimus ethanol-based formulation (TE) were switched to TCD and followed for 12 months. Assessments of efficacy and safety at baseline (TE) and month 12 (TCD) included concomitant corticosteroid use, distance best-corrected visual acuity, slit-lamp grading of conjunctival and corneal signs, Oxford staining, tear meniscus height (TMH), non-invasive break-up time, ocular redness, intraocular pressure, NEI VFQ-25 (National Eye Institute Visual Function Questionnaire) scores, symptom visual analog scales and adherence. In addition, a comparative evaluation of microbiological stability in use was performed for both eye drops.

Concomitant corticosteroids declined from 21.4 % to 5 %; two-thirds of eyes maintained or improved visual acuity; ≥80 % showed stable or improved (TMH p<0.0001) corneal/conjunctival. TMH increased significantly (median 0.25 to 0.29 mm; p<0.0001), while break-up time and intraocular pressure remained stable. VFQ-25 total score rose from 82.8 to 87.8 (p<0.001); burning, photophobia and foreign-body sensation decreased (p<0.05), thereby promoting adherence to treatment. Both tacrolimus formulations were similarly contaminated due to improper manipulation by the patients.

The 0.015 % tacrolimus/HPβCD formulation proves efficacy, and safety over 12 months for the treatment of diverse ocular inflammatory conditions, delivering sustained clinical stability and patient-reported benefits with reduced steroid reliance.