Instillation of ophthalmic formulation containing nilvadipine nanocrystals attenuates lens opacification in shumiya cataract rats

Ryoka Goto, Shigehiro Yamada, Hiroko Otake, Yosuke Nakazawa, Mikako Oka, Naoki Yamamoto, Hiroshi Sasaki, Noriaki Nagai

研究成果: Article査読

抄録

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.

本文言語English
論文番号1999
ジャーナルPharmaceutics
13
12
DOI
出版ステータスPublished - 2021 12月

ASJC Scopus subject areas

  • 薬科学

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