title: Lipid nanoparticles for prolonged topical delivery: an in vitro and in vivo investigation.
abstract: Dermal therapy is still a challenge due to the difficulties in controlling the active pharmaceutical ingredient (API) fate within the skin. Recently, lipid nanoparticles have shown a great potential as vehicle for topical administration of active substances, principally owing to the possible targeting effect and controlled release in different skin strata. Ketoprofen and naproxen loaded lipid nanoparticles were prepared, using hot high pressure homogenization and ultrasonication techniques, and characterized by means of photo correlation spectroscopy and differential scanning calorimetry. Nanoparticle behavior on human skin was assessed, in vitro, to determine drug percutaneous absorption (Franz cell method) and, in vivo, to establish the active localization (tape-stripping technique) and the controlled release abilities (UVB-induced erythema model). Results demonstrated that the particles were able to reduce drug penetration increasing, simultaneously, the permeation and the accumulation in the horny layer. A prolonged anti-inflammatory effect was observed in the case of drug loaded nanoparticles with respect to the drug solution. Direct as well as indirect evidences corroborate the early reports on the usefulness of lipid nanoparticles as carriers for topical administration, stimulating new and deeper investigations in the field.
authors.affiliation: Department of Pharmaceutical Sciences, School of Pharmacy, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Carmelo
authors.initials: C
authors.lastname: Puglia
authors.forename: Paolo
authors.initials: P
authors.lastname: Blasi
authors.forename: Luisa
authors.initials: L
authors.lastname: Rizza
authors.forename: Aurélie
authors.initials: A
authors.lastname: Schoubben
authors.forename: Francesco
authors.initials: F
authors.lastname: Bonina
authors.forename: Carlo
authors.initials: C
authors.lastname: Rossi
authors.forename: Maurizio
authors.initials: M
authors.lastname: Ricci
mesh_terms: D000287:Administration, Topical; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D005260:Female; D005782:Gels; D006801:Humans; D066298:In Vitro Techniques; D007660:Ketoprofen / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D008055:Lipids / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles; D009288:Naproxen / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D010316:Particle Size; D012867:Skin / Q000737:chemistry; D012869:Skin Absorption; D014465:Ultrasonics
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005782:Gels; D008055:Lipids; D009288:Naproxen; D007660:Ketoprofen