Abstract: Hesperetin (HST) exhibits antioxidant activity and helps prevent cataract formation when administered orally. However, low bioavailability limits its efficacy. However, formulating HST as an ophthalmic preparation may improve its delivery to ocular tissues, making it a more effective option for cataract prevention. In the present study, we prepared HST nanosuspensions (HST-NPs) and used a sodium selenite-induced cataract model to evaluate their anti-cataract efficacy. HST-NPs (1 % HST) were prepared using bead milling treatment and various additives (mannitol, parabens, methylcellulose, 2-hydroxypropyl-Β-cyclodextrin), and quantification of HST in samples was performed using high-performance liquid chromatography. HST in both suspensions HST-NPs (with bead milling) and HST-MPs (without bead milling) was in the crystalline state, and the mean particle size of HST-NPs was 174 nm. Moreover, the transcorneal penetration of HST-NPs was higher than that of HST-MPs. HST levels in lenses treated with HST-MPs were below the limit of detection, whereas HST was detectable in HST-NP-treated rats at both 30 and 120 min post-instillation. In addition, instillation of HST suspensions prevented lens opacification in rats with selenite-induced cataracts; HST-NPs significantly inhibited lens opacification compared with HST-MPs. In conclusion, we successfully designed HST-NPs with high corneal penetration and effective delivery into the lens and demonstrated that instillation of HST-NPs significantly prevented lens opacification in a selenite-induced cataract model compared with HST-MPs. These findings may contribute to future advances in the prevention of cataract development.
Mano et al. (Thu,) studied this question.