title: Development of mucoadhesive buccal films for the treatment of oral sub-mucous fibrosis: a preliminary study.
abstract: The objective of the present study was to develop the mucoadhesive buccal film of valdecoxib for the treatment of oral sub mucous fibrosis, a localized buccal disease. Valdecoxib, a novel COX-2 inhibitor has been reported to be used in various osteopathic and rheumatoid conditions as oral therapy. The films were made out of chitosan and HPMC K4M as polymers. Sodium taurocholate was used as a permeation enhancer. All the formulations were examined for film thickness, swelling properties, drug content, weight variation, in vitro release studies, bioadhesive force, tensile strength, diffusion studies using pig mucosa and pharmacokinetic study in healthy male volunteers. Prepared films were thin, flexible, smooth and transparent. Bioadhesive force and tensile strength of the optimized formulation were found to be 75 +/- 4 kg m(-1) S(-2) and more than 2.5 kg/3 cm(2), respectively. The percent drug content was 98.5 +/- 1.3%. The in vitro drug release from the selected formulation showed that about 69.34% of the drug payload was released up to 6 hours. The drug permeation through the dialysis sac and pig buccal mucosa was found to be 62.70% and 54.39%, respectively. Pharmacokinetic studies of the buccal mucoadhesive film showed that the drug was released locally at the target site of action, and a very small amount might have absorbed systemically.
authors.affiliation: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka State, India. ranjith.kumar@manipal.edu
authors.forename: Ranjith Kumar
authors.initials: RK
authors.lastname: Averineni
authors.forename: Subramanian Ganesa
authors.initials: SG
authors.lastname: Sunderajan
authors.forename: Srinivas
authors.initials: S
authors.lastname: Mutalik
authors.forename: Usha
authors.initials: U
authors.lastname: Nayak
authors.forename: Gopal
authors.initials: G
authors.lastname: Shavi
authors.forename: Karthik
authors.initials: K
authors.lastname: Armugam
authors.forename: Sreenivasa Reddy
authors.initials: SR
authors.lastname: Meka
authors.forename: Sureshwar
authors.initials: S
authors.lastname: Pandey
authors.forename: Udupa
authors.initials: U
authors.lastname: Nayanabhirama
mesh_terms: D000268:Adhesiveness; D000278:Administration, Buccal; D000328:Adult; D000818:Animals; D048271:Chitosan / Q000008:administration & dosage / Q000737:chemistry*; D016861:Cyclooxygenase Inhibitors / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D004058:Diffusion; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D006801:Humans; D065347:Hypromellose Derivatives; D007555:Isoxazoles / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D009061:Mouth Mucosa / Q000378:metabolism*; D009914:Oral Submucous Fibrosis / Q000188:drug therapy*; D013449:Sulfonamides / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D013552:Swine; D013656:Taurocholic Acid / Q000737:chemistry; D013718:Tensile Strength; D000096926:Benzenesulfonamides
chemical_list: D048271:Chitosan; D016861:Cyclooxygenase Inhibitors; D004337:Drug Carriers; D065347:Hypromellose Derivatives; D007555:Isoxazoles; D008747:Methylcellulose; D013449:Sulfonamides; D013656:Taurocholic Acid; C406224:valdecoxib; D000096926:Benzenesulfonamides