An <i>In Vitro</i> Evaluation for Corneal Damages after Instillation of Eye Drops Using Rat Debrided Corneal Epithelium: Changes in Corneal Damage of Benzalkonium Chloride by Addition of Thickening Agent

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  • Nagai Noriaki
    School of Pharmacy, Kinki University
  • Ito Yoshimasa
    School of Pharmacy, Kinki University Pharmaceutial Research and Technology Institute, Kinki University
  • Okamoto Norio
    Department of Ophthalmology, Kinki University School of Medicine
  • Shimomura Yoshikazu
    Department of Ophthalmology, Kinki University School of Medicine

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Other Title
  • ラット角膜上皮剥離モデルを用いた点眼薬の角膜傷害性評価:粘稠化剤添加に伴うベンザルコニウム塩化物角膜傷害性の変化
  • ラット カクマク ジョウヒ ハクリ モデル オ モチイタ テンガンヤク ノ カクマク ショウガイセイ ヒョウカ : ネンチュウカザイ テンカ ニ トモナウ ベンザルコニウム エンカブツ カクマク ショウガイセイ ノ ヘンカ

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Description

  Benzalkonium chloride (BAC) is known to cause corneal epithelial damage. In this study we investigated the effect of a BAC solution containing a thickening agent, which enhanced residence time in the eyes, on corneal wound healing using in vivo rat model debrided corneal epithelium. 0.5% or 1.0% methylcellulose (MC), carboxymethylcellulose (CMC) and hydroxypropyl-methylcellulose (HPMC) were used as the thickening agent. The levels of corneal wound healing of rat eyes injected with saline were alone approximately 45.0% at 12 h and 93.6% at 24 h after corneal epithelial abrasion, and healing was almost complete at 36 h. The healing rate in the rat eye treated just with MC, CMC and HPMC was higher than that in those injected with saline. In contrast to the treatment result using only this thickening agent, the healing rate in the eye treated with BAC was lower than that in those injected with saline: the corneal wounds in the BAC-treated eye showed approximately 20% healing at 12 h after abrasion. The injection of 0.02% BAC solution containing MC, CMC and HPMC more significantly delayed the healing than did the injection of 0.02% BAC alone. The results show that the in vivo evaluation method for corneal damage using rat debrided corneal epithelium reflects a toxic change depending upon residence time. These findings provide valuable safety and efficacy information for use in the design of eye drops.<br>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 132 (7), 837-843, 2012-07-01

    The Pharmaceutical Society of Japan

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