title: Poly[acrylonitrile-co-(N-vinyl pyrrolidone)] nanoparticles - Composition-dependent skin penetration enhancement of a dye probe and biocompatibility.
abstract: Nanoparticles can improve topical drug delivery: size, surface properties and flexibility of polymer nanoparticles are defining its interaction with the skin. Only few studies have explored skin penetration for one series of structurally related polymer particles with systematic alteration of material composition. Here, a series of rigid poly[acrylonitrile-co-(N-vinyl pyrrolidone)] model nanoparticles stably loaded with Nile Red or Rhodamin B, respectively, was comprehensively studied for biocompatibility and functionality. Surface properties were altered by varying the molar content of hydrophilic NVP from 0 to 24.1% and particle size ranged from 35 to 244nm. Whereas irritancy and genotoxicity were not revealed, lipophilic and hydrophilic nanoparticles taken up by keratinocytes affected cell viability. Skin absorption of the particles into viable skin ex vivo was studied using Nile Red as fluorescent probe. Whilst an intact stratum corneum efficiently prevented penetration, almost complete removal of the horny layer allowed nanoparticles of smaller size and hydrophilic particles to penetrate into viable epidermis and dermis. Hence, systematic variations of nanoparticle properties allows gaining insights into critical criteria for biocompatibility and functionality of novel nanocarriers for topical drug delivery and risks associated with environmental exposure.
authors.affiliation: Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany.
authors.forename: Nan
authors.initials: N
authors.lastname: Zhang
authors.affiliation: Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany.
authors.forename: André
authors.initials: A
authors.lastname: Said
authors.affiliation: Institute of Biomaterial Science and Berlin-Brandenburg Center for Regenerative Therapies, Helmholtz-Zentrum Geesthacht, Teltow, Germany; Helmholtz Virtual Institute Multifunctional Biomaterials for Medicine, Helmholtz-Zentrum Geesthacht, Teltow, Germany.
authors.forename: Christian
authors.initials: C
authors.lastname: Wischke
authors.affiliation: Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany.
authors.forename: Vivian
authors.initials: V
authors.lastname: Kral
authors.affiliation: Helmholtz Virtual Institute Multifunctional Biomaterials for Medicine, Helmholtz-Zentrum Geesthacht, Teltow, Germany; Institute of Physics, Freie Universität Berlin, Berlin, Germany.
authors.forename: Robert
authors.initials: R
authors.lastname: Brodwolf
authors.affiliation: Institute of Physics, Freie Universität Berlin, Berlin, Germany.
authors.forename: Pierre
authors.initials: P
authors.lastname: Volz
authors.affiliation: Institute of Physics, Freie Universität Berlin, Berlin, Germany.
authors.forename: Alexander
authors.initials: A
authors.lastname: Boreham
authors.affiliation: Institute of Nutritional Science, University of Potsdam, Germany.
authors.forename: Christian
authors.initials: C
authors.lastname: Gerecke
authors.affiliation: Institute of Biomaterial Science and Berlin-Brandenburg Center for Regenerative Therapies, Helmholtz-Zentrum Geesthacht, Teltow, Germany.
authors.forename: Wenzhong
authors.initials: W
authors.lastname: Li
authors.affiliation: Institute of Biomaterial Science and Berlin-Brandenburg Center for Regenerative Therapies, Helmholtz-Zentrum Geesthacht, Teltow, Germany; Helmholtz Virtual Institute Multifunctional Biomaterials for Medicine, Helmholtz-Zentrum Geesthacht, Teltow, Germany.
authors.forename: Axel T
authors.initials: AT
authors.lastname: Neffe
authors.affiliation: Institute of Nutritional Science, University of Potsdam, Germany.
authors.forename: Burkhard
authors.initials: B
authors.lastname: Kleuser
authors.affiliation: Helmholtz Virtual Institute Multifunctional Biomaterials for Medicine, Helmholtz-Zentrum Geesthacht, Teltow, Germany; Institute of Physics, Freie Universität Berlin, Berlin, Germany.
authors.forename: Ulrike
authors.initials: U
authors.lastname: Alexiev
authors.affiliation: Institute of Biomaterial Science and Berlin-Brandenburg Center for Regenerative Therapies, Helmholtz-Zentrum Geesthacht, Teltow, Germany; Helmholtz Virtual Institute Multifunctional Biomaterials for Medicine, Helmholtz-Zentrum Geesthacht, Teltow, Germany.
authors.forename: Andreas
authors.initials: A
authors.lastname: Lendlein
authors.affiliation: Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany; Helmholtz Virtual Institute Multifunctional Biomaterials for Medicine, Helmholtz-Zentrum Geesthacht, Teltow, Germany. Electronic address: Monika.Schaefer-Korting@fu-berlin.de.
authors.forename: Monika
authors.initials: M
authors.lastname: Schäfer-Korting
mesh_terms: D000181:Acrylonitrile / Q000008:administration & dosage / Q000737:chemistry*; D001672:Biocompatible Materials / Q000008:administration & dosage / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D004817:Epidermis / Q000378:metabolism*; D005456:Fluorescent Dyes / Q000008:administration & dosage / Q000737:chemistry*; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D015603:Keratinocytes / Q000378:metabolism; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D010078:Oxazines / Q000008:administration & dosage / Q000737:chemistry; D010316:Particle Size; D011108:Polymers / Q000008:administration & dosage / Q000737:chemistry; D011760:Pyrrolidinones / Q000008:administration & dosage / Q000737:chemistry*; D012869:Skin Absorption / Q000187:drug effects; D013499:Surface Properties
chemical_list: D001672:Biocompatible Materials; D004337:Drug Carriers; D005456:Fluorescent Dyes; D010078:Oxazines; D011108:Polymers; D011760:Pyrrolidinones; C042670:N-vinyl-2-pyrrolidinone; D000181:Acrylonitrile; C044808:nile red
keywords: Biocompatibility testing; Drug delivery systems; Nanoparticle; Poly[acrylonitrile-co-(N-vinyl pyrrolidone)]; Polymers; Skin absorption