title: Chitosan in mucoadhesive drug delivery: focus on local vaginal therapy.
abstract: Mucoadhesive drug therapy destined for localized drug treatment is gaining increasing importance in today's drug development. Chitosan, due to its known biodegradability, bioadhesiveness and excellent safety profile offers means to improve mucosal drug therapy. We have used chitosan as mucoadhesive polymer to develop liposomes able to ensure prolonged residence time at vaginal site. Two types of mucoadhesive liposomes, namely the chitosan-coated liposomes and chitosan-containing liposomes, where chitosan is both embedded and surface-available, were made of soy phosphatidylcholine with entrapped fluorescence markers of two molecular weights, FITC-dextran 4000 and 20,000, respectively. Both liposomal types were characterized for their size distribution, zeta potential, entrapment efficiency and the in vitro release profile, and compared to plain liposomes. The proof of chitosan being both surface-available as well as embedded into the liposomes in the chitosan-containing liposomes was found. The capability of the surface-available chitosan to interact with the model porcine mucin was confirmed for both chitosan-containing and chitosan-coated liposomes implying potential mucoadhesive behavior. Chitosan-containing liposomes were shown to be superior in respect to the simplicity of preparation, FITC-dextran load, mucoadhesiveness and in vitro release and are expected to ensure prolonged residence time on the vaginal mucosa providing localized sustained release of entrapped model substances.
authors.affiliation: Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Tromsø 9037, Norway. toril.andersen@uit.no.
authors.forename: Toril
authors.initials: T
authors.lastname: Andersen
authors.affiliation: Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Tromsø 9037, Norway. bleher.stefan@gmail.com.
authors.forename: Stefan
authors.initials: S
authors.lastname: Bleher
authors.affiliation: Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Tromsø 9037, Norway. goril.flaten@uit.no.
authors.forename: Gøril
authors.initials: G
authors.lastname: Eide Flaten
authors.affiliation: PharmaLuxLab Research Group, School of Pharmacy, Faculty of Mathematics and Natural Sciences, University of Oslo, 0316 Oslo, Norway. ingunn.tho@farmasi.uio.no.
authors.forename: Ingunn
authors.initials: I
authors.lastname: Tho
authors.affiliation: Department of Pharmacology and Clinical Neuroscience, Division of Clinical Pharmacology, Umeå University, Umeå SE-90187, Sweden. sofia.mattsson@pharm.umu.se.
authors.forename: Sofia
authors.initials: S
authors.lastname: Mattsson
authors.affiliation: Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Tromsø 9037, Norway. natasa.skalko-basnet@uit.no.
authors.forename: Nataša
authors.initials: N
authors.lastname: Škalko-Basnet
mesh_terms: D000268:Adhesiveness; D000282:Administration, Intravaginal; D048271:Chitosan / Q000494:pharmacology / Q000627:therapeutic use*; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage / Q000627:therapeutic use; D009092:Mucous Membrane / Q000378:metabolism; D010316:Particle Size; D014621:Vagina / Q000378:metabolism
chemical_list: D008081:Liposomes; D048271:Chitosan