title: In vitro Percutaneous Absorption of Niacinamide and Phytosterols and in vivo Evaluation of their Effect on Skin Barrier Recovery.
abstract: In this study, we evaluated different strategies to optimize the percutaneous absorption of niacinamide (NA) and soy phytosterols (FITO) by making use of solid lipid nanoparticles (SLN) and penetration enhancers, such as the hydrogenated lecithin. The evaluation of the skin permeation of NA and FITO has been effected in vitro using excised human skin (i.e., stratum corneum-epidermis or SCE). Furthermore, we evaluated the in vivo effect that NA and FITO has on skin barrier recovery after the topical application; using the extent of methyl nicotinate (MN)-induced erythema in damaged skin as a parameter to determine the rate of stratum corneum recovery. Results pointed out the importance of these strategies as valid tools for NA and FITO topical delivery. In fact, soy lecithin based formulations were able to increase the percutaneous absorption of the two active ingredients, while SLN guaranteed an interesting delayed and sustained release of FITO. In vivo evaluation showed clearly that the formulation containing both the actives (NA and FITO) is able to recover about 95% of skin barrier integrity eight days after tape stripping. This effect is probably due to the "synergistic effect" of NA and FITO.
authors.forename: Alessia
authors.initials: A
authors.lastname: Offerta
authors.forename: Francesco
authors.initials: F
authors.lastname: Bonina
authors.forename: Franco
authors.initials: F
authors.lastname: Gasparri
authors.forename: Andrea
authors.initials: A
authors.lastname: Zanardi
authors.forename: Lucia
authors.initials: L
authors.lastname: Micicche
authors.affiliation: Dept. of Drug Sciences University of Catania, Viale A. Doria 6, 95125 Catania, Italy. capuglia@unict.it.
authors.forename: Carmelo
authors.initials: C
authors.lastname: Puglia
mesh_terms: D000287:Administration, Topical; D000328:Adult; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D004817:Epidermis / Q000378:metabolism; D005260:Female; D006801:Humans; D054709:Lecithins / Q000737:chemistry; D008055:Lipids / Q000737:chemistry; D008297:Male; D053758:Nanoparticles / Q000737:chemistry; D009536:Niacinamide / Q000737:chemistry* / Q000378:metabolism*; D009539:Nicotinic Acids / Q000737:chemistry; D010539:Permeability; D010840:Phytosterols / Q000737:chemistry* / Q000378:metabolism*; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption
chemical_list: D004337:Drug Carriers; D054709:Lecithins; D008055:Lipids; D009539:Nicotinic Acids; D010840:Phytosterols; D009536:Niacinamide; C008473:methyl nicotinate