Role of chitosan on controlling the characteristics and antifungal activity of bioadhesive fluconazole vaginal tablets

• Main Authors: Rawan A. Fitaihi, Fadilah S. Aleanizy, Samar Elsamaligy, Hanaa A. Mahmoud, Mohsen A. Bayomi
• Format: Article
• Language: English
• Published: Elsevier 2018-02-01
• Series: Saudi Pharmaceutical Journal
• Subjects: Fluconazole; Chitosan; Bioadhesive polymers; Prolonged release; Swelling; Antifungal activity
• Online Access: http://www.sciencedirect.com/science/article/pii/S1319016417302244

Vaginal fluconazole (FLZ) prolonged release tablets containing chitosan in physical blends with other bioadhesive polymers were designed. Chitosan was mixed with hydroxypropyl methylcellulose (HPMC), guar gum or sodium carboxymethyl cellulose (NaCMC) at different ratios and directly compressed into tablets. In-vitro release profiles of FLZ were monitored at pH 4.8. Compressing chitosan with HPMC at different ratios slowed FLZ release, however, time for 80% drug release (T80) did not exceed 4.3 h for the slowest formulation (F11). Adding of chitosan to guar gum at 1:2 ratio (F3) showed delayed release with T80 17.4 h while, in presence of PVP at 1:2:1 ratio (F5), T80 was 8.8 h. A blend of chitosan and NaCMC at 1:2 ratio (F15) showed prolonged drug release with T80 11.16 h. Formulations F5 and F15 showed fair physical characteristics for the powder and tablets and were subjected to further studies. Fast swelling was observed for F15 that reached 1160.53 ± 13.02% in 4 h with 2 h bioadhesion time to mouse peritoneum membrane compared with 458.83 ± 7.09% swelling with bioadhesion time exceeding 24 h for F5. Extensive swelling of F15 could indicate possible dehydration effect on vaginal mucosa. Meanwhile, antifungal activity against C. albicans was significantly high for F5.