Prediction of Skin Permeation of Flurbiprofen from Neat Ester Oils and Their O/W Emulsions

• Todo Hiroaki

  Graduate School of Pharmaceutical Sciences, Josai University Faculty of Pharmacy and Pharmaceutical Sciences, Josai University

• Tamura Mai

  Graduate School of Pharmaceutical Sciences, Josai University

• Uchida Takashi

  R&D–Development Research, Kao Corporation

• Kurumada Miyuki

  Graduate School of Pharmaceutical Sciences, Josai University

• Motoki Anzu

  Graduate School of Pharmaceutical Sciences, Josai University

• Sano Tomohiko

  Faculty of Life and Environmental Sciences, Teikyo University of Science

• Onuki Yoshinori

  Department of Pharmaceutical Technology, Graduate School of Medical and Pharmaceutical Science, University of Toyama

• Takayama Kozo

  Faculty of Pharmacy and Pharmaceutical Sciences, Josai University

• Sugibayashi Kenji

  Graduate School of Pharmaceutical Sciences, Josai University Faculty of Pharmacy and Pharmaceutical Sciences, Josai University

書誌事項

タイトル別名

• Prediction of Skin Permeation of Flurbiprofen from Neat Ester Oils and Their <i>O</i>/<i>W</i> Emulsions

抄録

Although many in silico models were reported to predict the skin permeation of drugs from aqueous solutions, few studies were founded on the in silico estimation models for the skin permeation of drugs from neat oil formulations and o/w emulsions. In the present study, the cumulative amount of a model lipophilic drug, flurbiprofen (FP), that permeated through skin was determined from 12 different kinds of ester oils (Q_oil) and an in silico model was developed for predicting the skin permeation of FP from these ester oils. Thus, the obtained Q_oil values were well predicted with the FP solubility in the oils (S_oil), the amount of FP uptake into the stratum corneum (SC_oil) and molecular descriptors of dipolarity/polarizability (π₂^H) and molecular density. This model suggests that the thermodynamic activities of FP both in the formulations and skin are the key factors for predicting the skin permeation of FP from the ester oils. In addition, a high linear relationship was observed in the double-logarithm plots between the Q_oil and the cumulative amount of FP permeated through skin from 20% ester oil in water emulsion (Q_emul20%). Furthermore, the skin permeations of FP from 5 and 10% ester oil in water emulsions, Q_emul5% and Q_emul10%, respectively, were also predicted by the horizontal translation of the y-axis intercept of the liner equation for the relation between the Q_oil and Q_emul20%. These prediction methods must be helpful for designing topical oily and/or o/w emulsion formulations having suitable and high skin permeation rate of lipophilic drugs.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 66 (10), 959-966, 2018-10-01

  公益社団法人 日本薬学会

キーワード

• <i>in silico</i> prediction
• skin permeation
• ester oil
• oil in water emulsion
• Abraham descriptor

詳細情報

• CRID: 1390001288073563904
• NII論文ID: 130007492373
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.c18-00384
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 029238092
• PubMed: 30270242
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I029238092
• Web Site: https://www.jstage.jst.go.jp/article/cpb/66/10/66_c18-00384/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2019149486
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
  • KAKEN
• 抄録ライセンスフラグ: 使用不可