Fluconazole mucoadhesive buccal films: in vitro/in vivo performance.
Fluconazole mucoadhesive buccal films were prepared using film forming polymers namely; hydroxypropyl methyl cellulose (HPMC), hydroxyethyl cellulose (HEC), chitosan, Eudragit and sodium alginate (SALG) either alone or in combination with bioadhesive polymers. The bioadhesive polymers studied were sodium carboxymethyl cellulose (SCMC), Carbopol 974P, and polycarbophil (AA-A). The prepared films were characterized by means of film thickness, surface pH, swelling capacity, in vitro adhesion, in vivo residence time, in vitro drug release and in vivo drug release to determine the amount of drug release from selected film formulae using microbiological assay and HPLC. Optimum release behavior, convenient bioadhesion, acceptable elasticity were exhibited by film containing 2% HPMC and 1% SCMC (fresh or stored for 6 months). Determination of the amount of drug released in saliva after application of the selected fluconazole films confirmed the ability of the film to deliver the drug over a period of approximately 300 minutes and to reduce side effects and possibility of drug interaction encountered during systemic therapy of fluconazole, which would be beneficial in the case of oral candidiasis.
Department of Pharmaceutics, Faculty of Pharmacy, Cairo University Kasr El-Aini Street, Cairo, Egypt.
Soad A
SA
Yehia
Omaima N
ON
El-Gazayerly
Emad B
EB
Basalious
D000180:Acrylic Resins; D000268:Adhesiveness; D000328:Adult; D000464:Alginates / Q000008:administration & dosage; D000935:Antifungal Agents / Q000008:administration & dosage*; D002180:Candidiasis, Oral / Q000188:drug therapy; D002266:Carboxymethylcellulose Sodium / Q000008:administration & dosage; D002610:Cheek; D005260:Female; D015725:Fluconazole / Q000008:administration & dosage* / Q000737:chemistry; D020723:Glucuronic Acid / Q000008:administration & dosage; D006603:Hexuronic Acids / Q000008:administration & dosage; D006801:Humans; D065347:Hypromellose Derivatives; D008297:Male; D008747:Methylcellulose / Q000008:administration & dosage / Q000031:analogs & derivatives; D011145:Polyvinyls / Q000008:administration & dosage; D012995:Solubility
D000180:Acrylic Resins; D000464:Alginates; D000935:Antifungal Agents; D006603:Hexuronic Acids; D011145:Polyvinyls; C006912:carboxypolymethylene; D065347:Hypromellose Derivatives; D020723:Glucuronic Acid; D015725:Fluconazole; D008747:Methylcellulose; D002266:Carboxymethylcellulose Sodium