抄録
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.
