Formulation and In Vitro Characterization of Thiolated Buccoadhesive Film of Fluconazole

• Published in: AAPS PharmSciTech 2017-05, Vol.18 (4), p.1043-1055
• Main Authors: Naz, Kiran, Shahnaz, Gul, Ahmed, Naveed, Qureshi, Naveeda Akhtar, Sarwar, Hafiz Shoaib, Imran, Muhammad, Khan, Gul Majid
• Format: Article
• Language: English
• Subjects: Adhesives - chemistry; Adhesives - pharmacology; Administration, Buccal; Antifungal Agents - administration & dosage; Antifungal Agents - pharmacokinetics; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Carboxymethylcellulose Sodium - chemistry; Carboxymethylcellulose Sodium - pharmacology; Chitosan - chemistry; Chitosan - pharmacology; Cysteine - chemistry; Cysteine - pharmacology; Drug Delivery Systems - methods; Fluconazole - administration & dosage; Fluconazole - pharmacokinetics; Pharmacology/Toxicology; Pharmacy; Research Article; Sulfhydryl Compounds - chemistry; Sulfhydryl Compounds - pharmacology; Theme: Recent Trends in the Development of Chitosan-Based Drug Delivery Systems; Thioglycolates - chemistry; Thioglycolates - pharmacology
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-016-0607-y

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