title: Chitosan based nanoparticles functionalized with peptidomimetic derivatives for oral drug delivery.
abstract: The goal of this study was to develop an optimized drug delivery carrier for oral mucosa applications able to release in situ bioactive molecules by using biopolymeric materials. Among them chitosan and poly(lactic-co-glycolic acid) (PLGA) have gained considerable attention as biocompatible carriers able to improve the delivery of active agents. The formulation of such vehicles in the form of nanoparticles (NPs) could permit to exploit the peculiar properties of nanomaterials in order to enhance the efficacy of active agents. Chitosan (CS) and PLGA chlorexidine dihydrochloride (CHX)-loaded NPs were synthesized by ionotropic gelation and osmosis based methodology respectively. In order to facilitate NPs adhesion on human dental surfaces, two different strategies were employed: PLGA particles with an external shell of CS to produce a positive surface charge allowing CHX loaded PLGA NPs to interact with the negative charged dental surfaces, while CS particles were functionalized with peptidomimetic derivative glutathione (GSH). The morphology was investigated by scanning electron microscopy. A sustained release profile of CHX from CS NPs was achieved. CS-based NPs adhered on human tooth surfaces in a simulated brushing and rinsing process and their in vitro toxicity evaluation on Human Gingival Fibroblasts (HGFs) was between 20 and 60% in all experimental conditions. Thanks to their adhesion properties and low cytotoxicity, the synthesized CS-based formulations may be efficiently exploited for therapy purposes or to enhance in vivo dental care (i.e. preparation of toothpastes or other cosmetics for daily oral care).
authors.affiliation: Department of Chemistry, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Chronopoulou
authors.affiliation: Istituto di Biochimica e Biochimica Clinica, Università Cattolica del "Sacro Cuore", L.go F. Vito 1, 00168 Rome, Italy.
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Nocca
authors.affiliation: Istituto di Biochimica e Biochimica Clinica, Università Cattolica del "Sacro Cuore", L.go F. Vito 1, 00168 Rome, Italy.
authors.forename: Massimo
authors.initials: M
authors.lastname: Castagnola
authors.affiliation: Dipartimento di Scienze Chirurgiche della Testa e del Collo, Università Cattolica del "Sacro Cuore", L.go F. Vito 1, 00168 Rome, Italy.
authors.forename: Gaetano
authors.initials: G
authors.lastname: Paludetti
authors.affiliation: Department of Chemistry, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Giancarlo
authors.initials: G
authors.lastname: Ortaggi
authors.affiliation: Institute of Crystallography, Italian National Research Council (CNR), Bari 70126, Italy.
authors.forename: Fabio
authors.initials: F
authors.lastname: Sciubba
authors.affiliation: Department of Chemistry, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Melania
authors.initials: M
authors.lastname: Bevilacqua
authors.affiliation: Istituto di Chimica del Riconoscimento Molecolare, CNR, c/o Università Cattolica del "Sacro Cuore", L.go F. Vito 1, 00168 Rome, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Lupi
authors.affiliation: Department of Dental Sciences, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Gianluca
authors.initials: G
authors.lastname: Gambarini
authors.affiliation: Department of Chemistry, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy. Electronic address: cleofe.palocci@uniroma1.it.
authors.forename: Cleofe
authors.initials: C
authors.lastname: Palocci
mesh_terms: D000284:Administration, Oral; D000328:Adult; D002448:Cell Adhesion / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry / Q000494:pharmacology*; D002710:Chlorhexidine / Q000494:pharmacology; D016503:Drug Delivery Systems; D005978:Glutathione / Q000494:pharmacology; D006801:Humans; D057446:Hydrodynamics; D007700:Kinetics; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D057786:Peptidomimetics / Q000494:pharmacology*; D066244:Proton Magnetic Resonance Spectroscopy; D055672:Static Electricity; D014070:Tooth / Q000187:drug effects / Q000648:ultrastructure
chemical_list: D057786:Peptidomimetics; D048271:Chitosan; D005978:Glutathione; D002710:Chlorhexidine