【Original Contribution】Skin Permeation Enhancement of Bioactive Macromolecules by Reverse Micelles

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  • Kozaka Shuto
    Department of Applied Chemistry, Graduate School of Engineering, Kyushu University
  • Nakata Takahiro
    Kobayashi Pharmaceutical Co., Ltd.
  • Tajima Shiro
    Kobayashi Pharmaceutical Co., Ltd.
  • Ueda Taro
    Kobayashi Pharmaceutical Co., Ltd.
  • Goto Masahiro
    Department of Applied Chemistry, Graduate School of Engineering, Kyushu University Advanced Transdermal Drug Delivery System Center, Kyushu University

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Other Title
  • 【原著】逆ミセルによる高分子生理活性物質の経皮吸収促進
  • 逆ミセルによる高分子生理活性物質の経皮吸収促進
  • ギャクミセル ニ ヨル コウブンシ セイリ カッセイ ブッシツ ノ ケイヒ キュウシュウ ソクシン

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Abstract

Bioactive macromolecules are receiving great interest due to their versatile functions in living life, and especially, they have been extensively examined in medical application. In most cases, they are administered by mouth or injection, which accompanied with some drawbacks such as digestion in organs and the first–pass effect, etc. Although transdermal administration is a promising methodology that enables successful administration without these drawbacks, transdermal delivery of bioactive macromolecules is inhibited by a barrier function of Stratum Corneum (SC). To overcome the barrier function, we prepared reverse micelle formulation (RMF), in which bioactive macromolecules are encapsulated in reverse micelles. A model bioactive macromolecule, Heparinoid (HD), was successfully encapsulated inside the aqueous core of reverse micelles, and RMF was proven to be stable for more than 6 months at 40 ℃. RMF showed 100 times higher skin permeability of HD compared to its aqueous solution, which verifies the effectiveness of RMF as a transdermal administration carrier for bioactive macromolecules.

Journal

  • MEMBRANE

    MEMBRANE 44 (3), 130-135, 2019

    THE MEMBRANE SOCIETY OF JAPAN

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