title: Mucoadhesive vaginal tablets as veterinary delivery system for the controlled release of an antimicrobial drug, acriflavine.
abstract: The aim of the study was the development of mucoadhesive vaginal tablets designed for the local controlled release of acriflavine, an antimicrobial drug used as a model. The tablets were prepared using drug-loaded chitosan microspheres and additional excipients (methylcellulose, sodium alginate, sodium carboxymethylcellulose, or Carbopol 974). The microspheres were prepared by a spray-drying method, using the drug to polymer weight ratios 1:1 and 1:2 and were characterized in terms of morphology, encapsulation efficiency, and in vitro release behavior, as MIC (Minimum Inhibitory Concentration), MBC (Minimum Bacterial Concentration), and killing time (KT). The tablets were prepared by direct compression, characterized by in vitro drug release and in vitro mucoadhesive tests. The microparticles have sizes of 4 to 12 microm; the mean encapsulation yields are about 90%. Acriflavine, encapsulated into the polymer, maintains its antibacterial activity; killing time of the encapsulated drug is similar to that of the free drug. In vitro release profiles of tablets show differences depending on the excipient used. In particular Carbopol 974, which is highly cross-linked, is able to determine a drug-controlled release from the matrix tablets for more than 8 hours. The in vitro adhesion tests, carried out on the same formulation, show a good adhesive behavior. The formulation containing microspheres with drug to polymer weight ratios of 1:1 and Carbopol 974 is characterized by the best release behavior and shows good mucoadhesive properties. These preliminary data indicate that this formulation can be proposed as a mucoadhesive vaginal delivery system for the controlled release of acriflavine.
authors.affiliation: Dipartimento di Scienze del Farmaco, Università di Sassari, via Muroni 23/a, 07100 Sassari, Italy.
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Gavini
authors.forename: Vanna
authors.initials: V
authors.lastname: Sanna
authors.forename: Claudia
authors.initials: C
authors.lastname: Juliano
authors.forename: Maria Cristina
authors.initials: MC
authors.lastname: Bonferoni
authors.forename: Paolo
authors.initials: P
authors.lastname: Giunchedi
mesh_terms: D000167:Acriflavine / Q000737:chemistry*; D000179:Acrylates / Q000737:chemistry; D000268:Adhesiveness; D000282:Administration, Intravaginal; D000464:Alginates / Q000737:chemistry; D000818:Animals; D000891:Anti-Infective Agents, Local / Q000737:chemistry*; D001672:Biocompatible Materials / Q000737:chemistry; D001704:Biopolymers / Q000737:chemistry; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D002686:Chitin / Q000031:analogs & derivatives* / Q000737:chemistry; D048271:Chitosan; D003692:Delayed-Action Preparations / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods / Q000662:veterinary*; D016503:Drug Delivery Systems / Q000662:veterinary*; D005079:Excipients / Q000737:chemistry; D005260:Female; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D008855:Microscopy, Electron, Scanning / Q000379:methods; D008863:Microspheres; D013997:Time Factors; D014622:Vaginal Creams, Foams, and Jellies
chemical_list: D000179:Acrylates; D000464:Alginates; D000891:Anti-Infective Agents, Local; D001672:Biocompatible Materials; D001704:Biopolymers; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D006603:Hexuronic Acids; D014622:Vaginal Creams, Foams, and Jellies; C117167:carbopol 974P NF; D002686:Chitin; D000167:Acriflavine; D020723:Glucuronic Acid; D048271:Chitosan; D002266:Carboxymethylcellulose Sodium