title: A solid-in-oil nanodispersion for transcutaneous protein delivery.
abstract: Transcutaneous delivery attracts much attention but remains a challenging strategy for hydrophilic macromolecular drug administration. In the present study, we demonstrated that a solid-in-oil (S/O) nanodispersion, an oil-based nanodispersion of hydrophilic drugs, effectively enhanced the permeation of proteins into the skin. All of the different model proteins, FITC-labeled insulin (MW ca. 6 kDa), enhanced green fluorescent protein (EGFP, MW ca. 27 kDa) and horseradish peroxidase (HRP, MW ca. 40 kDa), permeated through the stratum corneum of Yucatan micropig skin in vitro by forming a S/O nanodispersion. The penetrated EGFP and HRP exhibited green fluorescence and catalytic activity, respectively, suggesting that these proteins can permeate into the skin in a functional form. The results indicated the potential utility of the S/O nanodispersion as a novel vehicle for transcutaneous protein delivery.
authors.affiliation: Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, 744 Moto-oka, Fukuoka 819-0395, Japan.
authors.forename: Yoshiro
authors.initials: Y
authors.lastname: Tahara
authors.forename: Shota
authors.initials: S
authors.lastname: Honda
authors.forename: Noriho
authors.initials: N
authors.lastname: Kamiya
authors.forename: Hongyu
authors.initials: H
authors.lastname: Piao
authors.forename: Akihiko
authors.initials: A
authors.lastname: Hirata
authors.forename: Eiji
authors.initials: E
authors.lastname: Hayakawa
authors.forename: Takeru
authors.initials: T
authors.lastname: Fujii
authors.forename: Masahiro
authors.initials: M
authors.lastname: Goto
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D016650:Fluorescein-5-isothiocyanate / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D049452:Green Fluorescent Proteins / Q000378:metabolism; D006735:Horseradish Peroxidase / Q000378:metabolism / Q000494:pharmacology; D066298:In Vitro Techniques; D007328:Insulin / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry; D009821:Oils / Q000008:administration & dosage / Q000378:metabolism*; D011506:Proteins / Q000008:administration & dosage / Q000378:metabolism*; D012867:Skin / Q000187:drug effects* / Q000378:metabolism*; D012869:Skin Absorption; D013552:Swine; D013556:Swine, Miniature
chemical_list: D007328:Insulin; D009821:Oils; D011506:Proteins; C485184:enhanced green fluorescent protein; C031573:insulin, fluorescein-isothiocyanated-; D049452:Green Fluorescent Proteins; D006735:Horseradish Peroxidase; D016650:Fluorescein-5-isothiocyanate