title: Vaginal inserts based on chitosan and carboxymethylcellulose complexes for local delivery of chlorhexidine: preparation, characterization and antimicrobial activity.
abstract: The aim of this work was to prepare vaginal inserts based on chitosan/carboxymethylcellulose polyelectrolyte complexes for local delivery of chlorhexidine digluconate. Complexes were prepared with different chitosan/carboxymethylcellulose molar ratios at a pH value close to pKa interval of the polymers and were characterized in terms of physico-chemical properties, complexation yield and drug loading. Then complexes were used to prepare inserts as vaginal dosage forms and their physical handling, morphology, water-uptake ability and drug release properties as well as antimicrobial activity toward Candida albicans and Escherichia coli were evaluated. Results confirmed the ionic interaction between chitosan and carboxymethylcellulose and the influence of the charge amount on the complexation yield. Complexes were characterized by high values of drug loading and showed increasing water-uptake ability with the increase of carboxymethylcellulose amount. The selection of appropriate chitosan/carboxymethylcellulose molar ratios allowed to obtain cone-like shaped solid inserts, easy to handle and able to hydrate releasing the drug over time. Finally, the formulated inserts showed antimicrobial activity against common pathogens responsible for vaginal infections.
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy. Electronic address: federica.bigucci@unibo.it.
authors.forename: Federica
authors.initials: F
authors.lastname: Bigucci
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy. Electronic address: angela.abruzzo2@unibo.it.
authors.forename: Angela
authors.initials: A
authors.lastname: Abruzzo
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy. Electronic address: b.vitali@unibo.it.
authors.forename: Beatrice
authors.initials: B
authors.lastname: Vitali
authors.affiliation: PolyCrystalLine s.r.l., Via F.S. Fabbri 127/1, Medicina, 40059 Bologna, Italy. Electronic address: bruno.saladini@polycristalline.it.
authors.forename: Bruno
authors.initials: B
authors.lastname: Saladini
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy. Electronic address: teresa.cerchiara2@unibo.it.
authors.forename: Teresa
authors.initials: T
authors.lastname: Cerchiara
authors.affiliation: Department of Chemistry and Chemical Technologies, University of Calabria, Via P. Bucci, Cubo 15D, Arcavacata di Rende, 87036 Cosenza, Italy. Electronic address: cate75@gmail.com.
authors.forename: Maria Caterina
authors.initials: MC
authors.lastname: Gallucci
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy. Electronic address: barbara.luppi@unibo.it.
authors.forename: Barbara
authors.initials: B
authors.lastname: Luppi
mesh_terms: D000282:Administration, Intravaginal; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage / Q000737:chemistry; D002176:Candida albicans / Q000187:drug effects / Q000254:growth & development; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry*; D048271:Chitosan / Q000737:chemistry*; D002710:Chlorhexidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D004304:Dosage Forms; D004339:Drug Compounding; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D014867:Water / Q000737:chemistry
chemical_list: D000891:Anti-Infective Agents, Local; D004304:Dosage Forms; D014867:Water; D048271:Chitosan; D002266:Carboxymethylcellulose Sodium; C010882:chlorhexidine gluconate; D002710:Chlorhexidine
keywords: Antimicrobial activity; Carboxymethylcellulose; Chitosan; Chlorhexidine digluconate; Polyelectrolyte complexes; Vaginal inserts