Formulation development and preclinical assessment of ethyl acetate fraction of Saraca asoca (EASA) flowers for cataract management.

BACKGROUND

Cataract is the leading cause of reversible blindness globally. Current treatment options are limited to surgical intervention, highlighting the need for pharmacological alternatives. The primary objective of this study was to develop an ocular formulation containing the ethyl acetate fraction of Saraca asoca (EASA) flowers and to evaluate the anti-cataract activity using in vitro, ex vivo and in vivo models.

METHODS

The EASA extract was characterized and analyzed by chromatographic techniques for the presence of phytoconstituents and the extract was formulated into an eye drop at 5 mg/mL. A comprehensive preclinical study evaluated the safety and efficacy of an ophthalmic formulation. Studies included in vitro antioxidant assays, in vitro irritation potential, ex vivo goat lens cataract model, in vivo ocular safety, in vivo diabetes, and UV-induced cataract models, affecting physiological enzymes and lens opacity.

RESULTS

Chromatographic analysis confirmed the presence of gallic acid, apigenin, and quercetin as key biomarkers from the EASA extract. The eye drop formulation produced a HET-CAM score of 0.5 (non-irritant) and the rabbit test showed no eye irritation up to 24 h. No abnormality or toxicity was observed after 28 days of ocular instillation. EASA exhibited significant antioxidant activity in DPPH, ABTS, FRAP assays and inhibited aldose reductase activity. Ex vivo studies of EASA demonstrated remarkable protection against lens opacification and in vivo treatment with EASA formulation preserved lens clarity compared to the negative control, while restoring endogenous antioxidants GSH, SOD and CAT to levels approaching those of normal controls.

CONCLUSION

Developed EASA eye drop formulation is non-irritant, ocularly safe, and displays potent antioxidant and aldose reductase inhibitory effects. EASA formulation significantly prevented and mitigated diabetes and UV-induced cataracts in preclinical models, supporting its potential as a non-invasive therapeutic option for cataract and ocular health management.