Characterization of a Riboflavin Non-aqueous Nanosuspension Prepared by Bead Milling for Cutaneous Application

• Sato Takayuki

  Graduate School of Pharmaceutical Sciences, Chiba University Pharmaceutics, Pharmaceutical Science Laboratories, Research Headquarters, Taisho Pharmaceutical Co., Ltd.

• Takeuchi Hiroyuki

  Pharmaceutics, Pharmaceutical Science Laboratories, Research Headquarters, Taisho Pharmaceutical Co., Ltd.

• Sakurai Takanobu

  Drug Safety, Drug Safety and Pharmacokinetics Laboratories, Research Headquarters, Taisho Pharmaceutical Co., Ltd.

• Tanaka Kensuke

  Pharmaceutics, Pharmaceutical Science Laboratories, Research Headquarters, Taisho Pharmaceutical Co., Ltd.

• Matsuki Kota

  Pharmaceutics, Pharmaceutical Science Laboratories, Research Headquarters, Taisho Pharmaceutical Co., Ltd.

• Higashi Kenjirou

  Graduate School of Pharmaceutical Sciences, Chiba University

• Moribe Kunikazu

  Graduate School of Pharmaceutical Sciences, Chiba University

• Yamamoto Keiji

  Graduate School of Pharmaceutical Sciences, Chiba University

抄録

The purpose of this study was to characterize the non-aqueous nanosuspension of a hydrophilic drug prepared by bead milling for cutaneous application. Riboflavin was used as the model hydrophilic drug. The non-aqueous nanosuspensions were prepared by grinding riboflavin with zirconia beads using eight non-aqueous bases. The mean particle size of riboflavin in the suspensions ranged from 206 to 469 nm, as determined by the dynamic light scattering method. Among the well-dispersed samples, riboflavin nanosuspension prepared in oleic acid was selected for evaluation of the drug permeability through rat skin. The cumulative amount and permeation rate of riboflavin from the nanosuspension were approximately three times higher than those for unprocessed riboflavin in oleic acid. Fluorescence imaging of the riboflavin nanosuspension suggested improved penetration of riboflavin into the stratum corneum. Furthermore, the addition of polysorbate 65 or polyglyceryl-6 polyricinoleate to the nanosuspension prepared in oleic acid markedly improved the riboflavin dispersibility. These results show that the preparation of a nanosuspension in a non-aqueous base by bead milling is one of the simple methods to improve the skin permeability of hydrophilic drugs.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 63 (2), 88-94, 2015

  公益社団法人 日本薬学会

キーワード

• bead milling
• riboflavin
• non-aqueous nanosuspension
• oleic acid
• stabilization
• skin permeability

詳細情報

• CRID: 1390001204178023936
• NII論文ID: 130004803766
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.c14-00641
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 026069321
• PubMed: 25748779
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I026069321
• Web Site: https://www.jstage.jst.go.jp/article/cpb/63/2/63_c14-00641/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2015307788
• 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