title: Formulation of polysaccharide-based nanoparticles for local administration into the oral cavity.
abstract: The efficacy of treatments for oral ailments is often challenged by a low residence time of the conventional pharmaceutical formulations in the oral cavity. The residence time in the oral cavity could be improved by using bioadhesive formulations, such as preparations based on polysaccharides. This study describes the formulation and the evaluation of polysaccharide-based nanosystems as drug delivery systems addressed to the oral cavity. Nanoparticles based on chitosan, alginate or pectin were prepared through self-assembly by ionotropic gelation using oppositely charged crosslinkers (tripolyphosphate or zinc). Characteristics of nanoparticles at increasing crosslinker concentration provided the basis for selecting the most suitable formulations. The nanoparticles were tested for cytotoxicity against buccal cells (TR146) and for stability in a medium simulating pH, ionic strength, electrolyte composition and concentration of saliva. Alginate nanoparticles were the most stable in the salivary environment, while chitosan nanoparticles were the most cytocompatible. Alginate nanoparticles and pectin nanoparticles revealed possible cytotoxicity due to the presence of zinc. This knowledge is important in the early design of polymer-based nanoparticles for oral usage and for potential improving of the biocompatibility of the investigated nanoparticles with the oral environment.
authors.affiliation: SiteDel Group, School of Pharmacy, University of Oslo, Norway; Nanobiotechnology Group, Institute of Plant Biology and Biotechnology, Westfälische Wilhelms-Universität Münster, Germany. Electronic address: sara.pistone@farmasi.uio.no.
authors.forename: Sara
authors.initials: S
authors.lastname: Pistone
authors.affiliation: Nanobiotechnology Group, Institute of Plant Biology and Biotechnology, Westfälische Wilhelms-Universität Münster, Germany. Electronic address: goycoole@uni-muenster.de.
authors.forename: Francisco M
authors.initials: FM
authors.lastname: Goycoolea
authors.affiliation: Department of Cariology and Gerodontology, Faculty of Dentistry, University of Oslo, Norway. Electronic address: a.y.vik@odont.uio.no.
authors.forename: Alix
authors.initials: A
authors.lastname: Young
authors.affiliation: SiteDel Group, School of Pharmacy, University of Oslo, Norway. Electronic address: gro.smistad@farmasi.uio.no.
authors.forename: Gro
authors.initials: G
authors.lastname: Smistad
authors.affiliation: SiteDel Group, School of Pharmacy, University of Oslo, Norway. Electronic address: marianne.hiorth@farmasi.uio.no.
authors.forename: Marianne
authors.initials: M
authors.lastname: Hiorth
mesh_terms: D000284:Administration, Oral; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D002626:Chemistry, Pharmaceutical; D006801:Humans; D009061:Mouth Mucosa / Q000187:drug effects* / Q000378:metabolism; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D011134:Polysaccharides / Q000008:administration & dosage* / Q000737:chemistry*
chemical_list: D011134:Polysaccharides
keywords: Artificial saliva; Cytotoxicity; Drug delivery; Ionic gelation; Nanoparticle; Oral cavity