Delay in ICR/f rat lens opacification by the instillation of eye drops containing disulfiram and hydroxypropyl-β-cyclodextrin inclusion complex

• Nagai Noriaki

  School of Pharmaceutical Sciences, Kinki University

• Takeda Maki

  School of Pharmaceutical Sciences, Kinki University

• Ito Yoshimasa

  School of Pharmaceutical Sciences, Kinki University Pharmaceutical Research and Tchnology Institute, Kinki University

• Takeuchi Noriko

  Section of Biochemistry, Faculty of Pharmacy, Meijo University

• Kamei Akira

  Section of Biochemistry, Faculty of Pharmacy, Meijo University

書誌事項

タイトル別名

• Delay in ICR/f Rat Lens Opacification by the Instillation of Eye Drops Containing Disulfiram and Hydroxypropyl-.BETA.-cyclodextrin Inclusion Complex
• Delay in ICR f rat lens opacification by the instillation of eye drops containing disulfiram and hydroxypropyl b cyclodextrin inclusion complex

抄録

In this study, we attempted to enhance disulfiram (DSF) solubility using a 2-hydroxypropyl-β-cyclodextrin (HPβCD) and hydroxypropylmethylcellulose (HPMC). We also investigated the effect of an HPβCD solution containing DSF and HPMC (DSF eye drops) on cataract development in ICR/f rat. The solubility of DSF increased with increasing HPβCD concentration, and the solubility of DSF in HPβCD solution containing 0.1% HPMC was approximately 20% greater than that of DSF in HPβCD solution without HPMC. In in vivo transcorneal penetration experiments using rabbits, only diethyldithiocarbamate (DDC) was detected (DSF was not detected) in the aqueous humor. This DSF-DDC conversion in the cornea was inhibited by treatment with a sulfhydryl (SH) inhibitor, p-mercuribenzoate and N-ethylmaleimide, in in vitro transcorneal penetration experiments using rabbit corneas. On the other hand, the instillation of 0.25% and 0.5% DSF eye drops delayed cataract development in ICR/f rats, a recessive-type hereditary cataractous strain. The present study demonstrates that DSF in HPβCD solution with HPMC is converted to DDC by the catalysis of proteins containing SH residues in the cornea, and this DDC may cause the delay in cataract development in ICR/f rats.

収録刊行物

• Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ

  Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 30 (8), 1529-1534, 2007

  公益社団法人 日本薬学会

キーワード

• cataract
• disulfiram
• 2-hydroxypropyl-β-cyclodextrin
• hydroxypropylmethylcellulose
• ICR/f rat

詳細情報

• CRID: 1390001204624314880
• NII論文ID: 110006366812
• NII書誌ID: AA10885497
• DOI: 10.1248/bpb.30.1529
• COI: 1:CAS:528:DC%2BD2sXhtFWmu73K
• ISSN: 13475215
• ISSN: 09186158
• NDL書誌ID: 8824854
• PubMed: 17666815
• Web Site: http://id.ndl.go.jp/bib/8824854
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I8824854
• Web Site: http://www.jstage.jst.go.jp/article/bpb/30/8/30_8_1529/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2008048530
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可