Abstract
We developed ophthalmic formulations based on nilvadipine (NIL) nanocrystals (NIL-NP dispersions; mean particle size: 98 nm) by using bead mill treatment and investigated whether the instillation of NIL-NP dispersions delivers NIL to the lens and prevents lens opacification in hereditary cataractous Shumiya cataract rats (SCRs). Serious corneal stimulation was not detected in either human corneal epithelial cells or rats treated with NIL-NP dispersions. The NIL was directly delivered to the lens by the instillation of NIL-NP dispersions, and NIL content in the lenses of rats instilled with NIL-NP dispersions was significantly higher than that in the ophthalmic formulations based on NIL microcrystals (NIL-MP dispersions; mean particle size: 21 µm). Moreover, the supply of NIL prevented increases in Ca2+ content and calpain activity in the lenses of SCRs and delayed the onset of cataracts. In addition, the anti-cataract effect in the lens of rats instilled with NIL-NP dispersions was also significantly higher than that in NIL-MP dispersions. NIL-NPs could be used to prevent lens opacification.
Highlights
Cataracts lead to impaired vision via partial or complete opacification of the lens, resulting in blindness
The diffractogram does not change with or without bead mill treatment. These results show that milled NIL has a crystalline arrangement, and the crystalline arrangement was not changed by the bead mill treatment
The addition of HPβCD enhanced the solubility of NIL, and the solubility in the NIL-MPs with HPβCD was 2.2-fold higher than the NIL-MPs without HPβCD
Summary
Cataracts lead to impaired vision via partial or complete opacification of the lens, resulting in blindness. Cataracts can be treated with the surgical replacement of the opacified lens, this surgery is not performed in developing countries. Due to a lack of access to eye care and complications associated with surgery, alternative treatments and treatment strategies using topical drugs, such as eye drops, are required to treat patients facing the threat of blindness. Increasing age, ultraviolet light, oxidative stress, lipid peroxidation, diabetes, the oxidation of lens proteins, genetic predispositions, and various toxic agents are known as risk factors for cataract formation [2,3,4,5,6]. Changes in the intracellular calcium ion (Ca2+ ) have long been known to be related to lens opacification, and the highest Ca2+
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