title: Bioadhesive properties of Gantrez nanoparticles.
abstract: Bioadhesive nanoparticles have been proposed as carriers for the oral delivery of poorly available drugs and facilitate the use of this route. This work summarises some experiments describing the bioadhesive potential of Gantrez nanoparticles fluorescently labeled with rhodamine B isothiocyanate. The adhesive potential of Gantrez was found to be stronger when folded as nanoparticles than in the solubilised form. Conventional nanoparticles displayed a tropism for the upper areas of the gastrointestinal tract, with a maximum of adhesion 30 min post-administration and a decrease in the adhered fraction along the time depending on the given dose. The cross-linkage of nanoparticles with increasing amounts of 1,3-diaminopropane stabilised the resulting carriers and prolonged their half-life in an aqueous environment; although, the adhesive capacity of nanoparticles, the intensity and the relative duration of the adhesive interactions within the gut as a function of the cross-linking degree. Finally, nanoparticles were coated with either gelatin or albumin. In the first case, the presence of gelatin dramatically decreased the initial capacity of these carriers to interact with the gut mucosa and the intensity of these phenomenons. In the latter, bovine serum albumin coated nanoparticles (BSA-NP) showed an important tropism for the stomach mucosa without further significant distribution to other parts of the gut mucosa.
authors.affiliation: Centro Galénico, Universidad de Navarra, 31080 - Pamplona (Spain). jmirache@unav.es
authors.forename: Juan M
authors.initials: JM
authors.lastname: Irache
authors.forename: María
authors.initials: M
authors.lastname: Huici
authors.forename: Monica
authors.initials: M
authors.lastname: Konecny
authors.forename: Socorro
authors.initials: S
authors.lastname: Espuelas
authors.forename: Miguel Angel
authors.initials: MA
authors.lastname: Campanero
authors.forename: Pau
authors.initials: P
authors.lastname: Arbos
mesh_terms: D000268:Adhesiveness; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D005753:Gastric Mucosa / Q000378:metabolism; D007413:Intestinal Mucosa / Q000378:metabolism; D008298:Maleates / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D008954:Models, Biological; D008968:Molecular Conformation; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D011145:Polyvinyls / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D013499:Surface Properties
chemical_list: D008298:Maleates; D011108:Polymers; D011145:Polyvinyls; C058026:polyvinylmethoxyethylene-maleic anhydride copolymer