title: Dermal absorption behavior of fluorescent molecules in nanoparticles on human and porcine skin models.
abstract: The percutaneous passage of poorly skin absorbed molecules can be improved using nanocarriers, particularly biodegradable polymeric nanospheres (NSs) or nanocapsules (NCs). However, penetration of the encapsulated molecules may be affected by other factors than the nanocarrier properties. To gain insight information on the skin absorption of two fluorescent cargos, DiIC18(5) and coumarin-6 were incorporated in NSs or NCs and topically applied on various human and porcine skin samples. 3D imaging techniques suggest that NSs and NCs enhanced deep dermal penetration of both probes similarly, when applied on excised human skin irrespective of the nature of the cargo. However, when ex vivo pig skin was utilized, the cutaneous absorption of DiIC18(5) was more pronounced by means of PLGA NCs than NSs. In contrast, PLGA NSs noticeably improved the porcine skin penetration of coumarin-6, as compared to the NCs. Furthermore, the porcine skin results were reproducible when triplicated whereas from various human skin samples, as expected, the results were not sufficiently reproducible and large deviations were observed. The overall findings from this comprehensive comparison emphasize the potential of PLGA NCs or NSs to promote cutaneous bioavailability of encapsulated drugs, exhibiting different physicochemical properties but depending on the nature of the skin.
authors.affiliation: Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 9112102, Israel.
authors.forename: Nir
authors.initials: N
authors.lastname: Debotton
authors.affiliation: Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 9112102, Israel.
authors.forename: Amit
authors.initials: A
authors.lastname: Badihi
authors.affiliation: Plastic Surgeon, Assaf Harofeh Medical Center, 69710, Tel Aviv, Israel.
authors.forename: Mano
authors.initials: M
authors.lastname: Robinpour
authors.affiliation: Department of Dermatology, Hadassah Medical Organization, The Hebrew University Medical School, Jerusalem 91010, Israel.
authors.forename: Claes D
authors.initials: CD
authors.lastname: Enk
authors.affiliation: Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 9112102, Israel. Electronic address: simonb@ekmd.huji.ac.il.
authors.forename: Simon
authors.initials: S
authors.lastname: Benita
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002232:Carbocyanines / Q000378:metabolism; D003374:Coumarins / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry*; D005456:Fluorescent Dyes / Q000378:metabolism*; D006801:Humans; D053769:Nanocapsules / Q000737:chemistry*; D054118:Nanospheres / Q000737:chemistry*; D012867:Skin; D012869:Skin Absorption; D013552:Swine
chemical_list: D002232:Carbocyanines; D003374:Coumarins; D004337:Drug Carriers; D005456:Fluorescent Dyes; D053769:Nanocapsules; C024286:3,3'-dioctadecylindocarbocyanine
keywords: Human; Nanocapsules; Nanospheres; Penetration; Porcine; Skin