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

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Article number1999
JournalPharmaceutics
Volume13
Issue number12
DOIs
Publication statusPublished - 2021 Dec

Keywords

  • Cataract
  • Nanocrystals
  • Nilvadipine
  • Ophathalmic formulation
  • Shumiya cataract rat

ASJC Scopus subject areas

  • Pharmaceutical Science

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