title: Bioadhesive properties and biodistribution of cyclodextrin-poly(anhydride) nanoparticles.
abstract: This work describes the preparation, characterization and evaluation of the nanoparticles formed by the copolymer of methyl vinyl ether and maleic anhydride (Gantrez) AN) and cyclodextrins, including beta-cyclodextrin (CD) hydroxypropyl-beta-cyclodextrin (HPCD) and 6-monodeoxy-6-monoamino-beta-cyclodextrin (NHCD). The cyclodextrin-poly(anhydride) nanoparticles were prepared by a solvent displacement method and characterized by measuring the size, zeta potential, morphology and composition. For bioadhesion studies, nanoparticles were fluorescently labelled with rhodamine B isothiocianate (RBITC). For in vivo imaging biodistribution studies, (99m)Tc-labelled nanoparticles were used. Nanoparticles displayed a size of about 150nm and a cyclodextrin content which was found optimal under the following experimental conditions: cyclodextrin/poly(anhydride) ratio of 0.25 by weight, 30min of incubation time between the cyclodextrin and the polymer. Moreover, the oligosaccharide content was higher with CD than with NHCD and HPCD. Overall, cyclodextrin-poly(anhydride) nanoparticles displayed homogeneous bioadhesive interactions within the gut. The intensity of these interactions was higher than for control nanoparticles. The high bioadhesive capacity was observed for HPCD-NP and NHCD-NP which can be related with their rough morphology and, thus, a higher specific surface than for smooth nanoparticles (CD-NP). Finally, from in vivo studies, no evidence of translocation of distribution to other organs was observed when these nanoparticles were orally administered.
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, University of Navarra, Apartado 177, 31008 Pamplona, Spain.
authors.forename: Maite
authors.initials: M
authors.lastname: Agüeros
authors.forename: Paloma
authors.initials: P
authors.lastname: Areses
authors.forename: Miguel Angel
authors.initials: MA
authors.lastname: Campanero
authors.forename: Hesham
authors.initials: H
authors.lastname: Salman
authors.forename: Gemma
authors.initials: G
authors.lastname: Quincoces
authors.forename: Ivan
authors.initials: I
authors.lastname: Peñuelas
authors.forename: Juan Manuel
authors.initials: JM
authors.lastname: Irache
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000269:Adhesives; D000818:Animals; D003505:Cyclodextrins / Q000737:chemistry* / Q000493:pharmacokinetics*; D004337:Drug Carriers; D004563:Electrochemistry; D005456:Fluorescent Dyes; D005772:Gastrointestinal Transit; D007553:Isotope Labeling; D007700:Kinetics; D008297:Male; D008299:Maleic Anhydrides; D008855:Microscopy, Electron, Scanning; D008856:Microscopy, Fluorescence; D053758:Nanoparticles; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012235:Rhodamines; D013667:Technetium; D014018:Tissue Distribution; D047392:beta-Cyclodextrins
chemical_list: D000269:Adhesives; D003505:Cyclodextrins; D004337:Drug Carriers; D005456:Fluorescent Dyes; D008299:Maleic Anhydrides; D012235:Rhodamines; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D013667:Technetium; C027755:rhodamine isothiocyanate