title: Skin delivery by block copolymer nanoparticles (block copolymer micelles).
abstract: Block copolymer nanoparticles often referred to as "block copolymer micelles" have been assessed as carriers for skin delivery of hydrophobic drugs. Such carriers are based on organic biocompatible and biodegradable materials loaded with hydrophobic drugs: poly(lactide)-block-poly(ethylene glycol) copolymer (PLA-b-PEG) nanoparticles that have a solid hydrophobic core made of glassy poly(d,l-lactide), and poly(caprolactone)-block-poly(ethylene glycol) copolymer (PCL-b-PEG) nanoparticles having a liquid core of polycaprolactone. In vitro skin absorption of all-trans retinol showed a large accumulation of retinol in stratum corneum from both block copolymer nanoparticles, higher by a factor 20 than Polysorbate 80 surfactant micelles and by a factor 80 than oil solution. Additionally, skin absorption from PLA-b-PEG nanoparticles was higher by one order of magnitude than PCL-b-PEG, although their sizes (65nm) and external surface (water-swollen PEG layer) were identical as revealed by detailed structural characterizations. Fluorescence microscopy of histological skin sections provided a non-destructive picture of the storage of Nile Red inside stratum corneum, epidermis and dermis. Though particle cores had a different physical states (solid or liquid as measured by (1)H NMR), the ability of nanoparticles for solubilization of the drug assessed from their Hildebrand solubility parameters appeared the parameter of best relevance regarding skin absorption.
authors.affiliation: Université Lyon 1, Laboratoire d'Automatique et de Génie des Procédés, CNRS UMR 5007, 43 bd 11 Novembre, 69622 Villeurbanne, France.
authors.forename: Faiza
authors.initials: F
authors.lastname: Laredj-Bourezg
authors.affiliation: Université Lyon 1, Laboratoire d'Automatique et de Génie des Procédés, CNRS UMR 5007, 43 bd 11 Novembre, 69622 Villeurbanne, France.
authors.forename: Marie-Alexandrine
authors.initials: MA
authors.lastname: Bolzinger
authors.affiliation: Université Lyon 1, Laboratoire d'Automatique et de Génie des Procédés, CNRS UMR 5007, 43 bd 11 Novembre, 69622 Villeurbanne, France.
authors.forename: Jocelyne
authors.initials: J
authors.lastname: Pelletier
authors.affiliation: Université Lyon 1, Laboratoire d'Automatique et de Génie des Procédés, CNRS UMR 5007, 43 bd 11 Novembre, 69622 Villeurbanne, France.
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Valour
authors.affiliation: Université Lyon 1, Laboratoire des Substituts Cutanés, CNRS FRE 3310, Hôpital Édouard Herriot, Lyon, France.
authors.forename: Marie-Rose
authors.initials: MR
authors.lastname: Rovère
authors.affiliation: Université Lyon 1, Centre d'Imagerie Quantitative Lyon-Est, Lyon, France.
authors.forename: Batoule
authors.initials: B
authors.lastname: Smatti
authors.affiliation: Université Lyon 1, Laboratoire d'Automatique et de Génie des Procédés, CNRS UMR 5007, 43 bd 11 Novembre, 69622 Villeurbanne, France. Electronic address: chevalier@lagep.univ-lyon1.fr.
authors.forename: Yves
authors.initials: Y
authors.lastname: Chevalier
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems; D005260:Female; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D012867:Skin / Q000378:metabolism*; D012995:Solubility; D013552:Swine
chemical_list: D008823:Micelles; D011091:Polyesters; C016240:polycaprolactone; D011092:Polyethylene Glycols; C033616:poly(lactide)
keywords: Block copolymer; Cutaneous absorption; Nanoparticle; Skin delivery