title: Formulation and In Vitro Characterization of Thiolated Buccoadhesive Film of Fluconazole.
abstract: The present work is focused on the development of thiolated film for fluconazole buccal delivery. To this end, unmodified polymers chitosan and sodium carboxymethylcellulose (NaCMC) backbone was covalently modified by thioglycolic acid (TGA) and cysteine, respectively. The thiolated buccoadhesive film was evaluated in terms of thickness, weight uniformity, water-uptake capacity, drug content, and release patterns. Moreover, mucoadhesion profile was investigated on buccal mucosa. The resulting chitosan-TGA and NaCMC-cysteine conjugates displayed 171 ± 13 and 380 ± 19 μmol thiol groups per gram of polymer (mean ± SD; n = 3), respectively. The water binding capacity of the thiolated film was significantly ∼2-fold higher (p < 0.05) as compared to unmodified film. The obtained thiolated film displayed 5.8-fold higher mucoadhesive properties compared with corresponding film. Controlled release of drugs from film was observed over 8 h. The transport of fluconazole across excised buccal mucosa was enhanced up to 17-fold in comparison with fluconazole applied in buffer. Based on these findings, thiolated film seems to be promising for fluconazole buccal delivery.
authors: Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
authors: Kiran
authors: K
authors: Naz
authors: Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan. gshahnaz@qau.edu.pk.
authors: Gul
authors: G
authors: Shahnaz
authors: Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
authors: Naveed
authors: N
authors: Ahmed
authors: Department of Animal Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
authors: Naveeda Akhtar
authors: NA
authors: Qureshi
authors: Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
authors: Hafiz Shoaib
authors: HS
authors: Sarwar
authors: Riphah Institute of Pharmaceutical Sciences 7th avenue G-7/4, Riphah International University, Islamabad, Pakistan.
authors: Muhammad
authors: M
authors: Imran
authors: Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
authors: Gul Majid
authors: GM
authors: Khan
mesh_terms: D000269:Adhesives / Q000737:chemistry / Q000494:pharmacology; D000278:Administration, Buccal; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry / Q000494:pharmacology; D048271:Chitosan / Q000737:chemistry / Q000494:pharmacology; D003545:Cysteine / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D015725:Fluconazole / Q000008:administration & dosage / Q000493:pharmacokinetics; D013438:Sulfhydryl Compounds / Q000737:chemistry / Q000494:pharmacology; D013864:Thioglycolates / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000269:Adhesives; D000935:Antifungal Agents; D013438:Sulfhydryl Compounds; D013864:Thioglycolates; C017487:2-mercaptoacetate; D015725:Fluconazole; D048271:Chitosan; D002266:Carboxymethylcellulose Sodium; D003545:Cysteine
keywords: buccal delivery; controlled release; mucoadhesion; polymeric buccoadhesive film; thiolated polymers