title: Chitosan/alginate complexes for vaginal delivery of chlorhexidine digluconate.
abstract: Chitosan/alginate complexes were prepared at different polycation/polyanion molar ratios and freeze-dried vaginal inserts were obtained for chlorhexidine digluconate local delivery in genital infections. Complex yield, FT-IR spectra, and TGA thermograms were studied to confirm the interaction between the two polyions. The influence of different complexes on physical handling, morphology, and drug distribution in the samples were evaluated by friability test, scanning electron microscopy (SEM), and energy dispersive X-ray spectroscopy (EDS), respectively. In vitro water-uptake, mucoadhesion and release tests were performed as well as microbiological tests toward pathogenic vaginal microorganisms. The results showed that the selection of suitable chitosan/alginate molar ratio and drug loading allowed modulate insert ability to hydrate, adhere to the mucosa, and release chlorhexidine digluconate. The insert containing an excess of alginate was found to be the best performing formulation and showed good antimicrobial activity toward the pathogens Candida albicans and Escherichia coli.
authors.affiliation: Department of Pharmaceutical Sciences, Via San Donato 19/2, University of Bologna, 40127 Bologna, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Abruzzo
authors.forename: F
authors.initials: F
authors.lastname: Bigucci
authors.forename: T
authors.initials: T
authors.lastname: Cerchiara
authors.forename: B
authors.initials: B
authors.lastname: Saladini
authors.forename: M C
authors.initials: MC
authors.lastname: Gallucci
authors.forename: F
authors.initials: F
authors.lastname: Cruciani
authors.forename: B
authors.initials: B
authors.lastname: Vitali
authors.forename: B
authors.initials: B
authors.lastname: Luppi
mesh_terms: D000268:Adhesiveness; D000282:Administration, Intravaginal; D000464:Alginates / Q000737:chemistry*; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage*; D002176:Candida albicans / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry*; D002710:Chlorhexidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D016503:Drug Delivery Systems; D004926:Escherichia coli / Q000187:drug effects; D005260:Female; D005831:Genital Diseases, Female / Q000188:drug therapy*; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006801:Humans; D008855:Microscopy, Electron, Scanning; D009092:Mucous Membrane / Q000187:drug effects / Q000378:metabolism; D013052:Spectrometry, X-Ray Emission; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D000464:Alginates; D000891:Anti-Infective Agents, Local; D006603:Hexuronic Acids; D020723:Glucuronic Acid; D048271:Chitosan; C010882:chlorhexidine gluconate; D002710:Chlorhexidine