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

Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society
Rawan A FitaihiMohsen A Bayomi

Abstract

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 ...Continue Reading

Citations

Jan 3, 2020·Drug Development and Industrial Pharmacy·Rita Solange Monteiro MachadoRita Palmeira-de-Oliveira
May 14, 2020·Pharmaceutical Development and Technology·Amal S M Abu El-EninMarwa Ahmed Fouad Lotfy
Apr 26, 2020·Journal of Clinical Medicine·Magdalena PaczkowskaJudyta Cielecka-Piontek
Mar 27, 2021·Carbohydrate Polymers·Victor Hugo Sousa AraujoMarlus Chorilli
Nov 7, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Wei-Hsuan LoChing-Hsuan Lin
Jan 21, 2021·Drug Delivery and Translational Research·Ana Carolina S RéTaís Gratieri

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