title: Efficient skin permeation of soluble proteins via flexible and functional nano-carrier.
abstract: In spite of several intrinsic and distinct advantages, a topical and transdermal administration of drugs has been limited mainly due to very low permeability of drugs across skin. Especially, it is generally regarded that hydrophilic macromolecules such as proteins, peptides, and vaccines cannot penetrate across skin. In this study, we demonstrated that chitosan-conjugated, Pluronic-based nano-carrier (nanogel) can act as an efficient delivery vehicle of hydrophilic proteins across human skin. The functional nano-carrier (<100 nm in size), chemically-crosslinking Pluronic F 127 with chitosan conjugation, is flexible and soft with reservoir characteristics for biomacromolecules. The in-vitro permeation experiments through human cadaver skin revealed remarkable permeability of hydrophilic proteins of various sizes including FITC-BSA (67 kDa) and FITC-Insulin (6 kDa) by direct penetration of the nano-carrier across skin. The bioactivity post-permeation of proteins via the functional nano-carrier was also confirmed by delivering ß-galactosidase. Results presented in this paper suggest the use of chitosan-conjugated flexible nano-carrier as a novel platform for transcutaneous delivery of hydrophilic macromolecules and other drug-delivery applications.
authors.affiliation: School of Materials Science and Engineering and Department of Nanobio Materials and Electronics, Gwangju Institute of Science and Technology, 261 Cheomdan-gwagiro, Buk-gu, Gwangju 500-712, South Korea.
authors.forename: Won Il
authors.initials: WI
authors.lastname: Choi
authors.forename: Jong Hyun
authors.initials: JH
authors.lastname: Lee
authors.forename: Ja-Young
authors.initials: JY
authors.lastname: Kim
authors.forename: Jin-Chul
authors.initials: JC
authors.lastname: Kim
authors.forename: Young Ha
authors.initials: YH
authors.lastname: Kim
authors.forename: Giyoong
authors.initials: G
authors.lastname: Tae
mesh_terms: D000279:Administration, Cutaneous; D048271:Chitosan / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D016650:Fluorescein-5-isothiocyanate / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D066298:In Vitro Techniques; D007328:Insulin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D008297:Male; D008875:Middle Aged; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry; D010539:Permeability; D020442:Poloxamer / Q000008:administration & dosage* / Q000737:chemistry; D012710:Serum Albumin, Bovine / Q000008:administration & dosage* / Q000737:chemistry; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption
chemical_list: D004337:Drug Carriers; D007328:Insulin; C039217:fluorescein isothiocyanate bovine serum albumin; C031573:insulin, fluorescein-isothiocyanated-; D020442:Poloxamer; D012710:Serum Albumin, Bovine; D048271:Chitosan; D016650:Fluorescein-5-isothiocyanate