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Purpose A new gel formulation of loteprednol etabonate (LE) has been developed which is non-settling, provides a pH close to physiological, and a reduced level of benzalkonium chloride. This study sought to examine the levels of LE in tear fluid following a single topical instillation of LE ophthalmic gel 0.5% to healthy volunteers. Methods Single center, open label study. Twelve healthy subjects received LE ophthalmic gel 0.5% in one eye and tear sampling was performed at 6 hours (h), 9 h, 12 h, and 24 h after instillation. LE levels in tears were determined by LC-MS/MS. Ocular and non-ocular treatment emergent adverse events (AEs) were recorded. Results 17 subjects were screened and 12 were enrolled. Mean age was 46 years and all but one subject was male. LE was detected in all tear fluid samples at all time points assessed. Mean (SD) LE levels were 114 (116) µg/g at 6 h, 19.7 (18.2) µg/g at 9 h, 26.9 (29.6) µg/g at 12 h and 2.41 (3.36) µg/g at 24 h. No drug-related AEs were reported. Conclusion LE administered in the gel formulation remains present in tear fluid 24 hours after a single instillation. These results suggest a long residency time of LE on the ocular surface with the gel formulation. No safety concerns were identified. Commercial interest |
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