Mucoadhesive tablets for oral administration of ciclopiroxolamine

Overview

Oral mucoadhesive tablets belong to modern dosage forms, which allow controlled drug release after buccal application. They are used for the treatment of oral cavity disorders or for systemic administration of drugs with high first-pass effect or drugs instable in gastrointestinal tract. This study reports the development of oral mucoadhesive tablets containing antimycotic drug ciclopiroxolamine. Mucoadhesive properties of placebo tablets containing different ratios of carbomer and hydroxypropylmethylcellulose were evaluated in vivo in healthy human volunteers. The longest mucoadhesion for 9 hours was achieved in matrices containing 60 % (w/w) of carbomer. When optimum combination of the two mucoadhesive polymers was selected, tablets containing ciclopiroxolamine were prepared and one tablet side was film-coated to make the application procedure easier. Tablet quality parameters were determined and drug dissolution profile was evaluated under different pH conditions. In vitro release of ciclopiroxolamine was slower than the desintegration of prepared mucoadhesive tablets in vivo. Nevertheless, tablets containing 25 mg of ciclopiroxolamine performed prolonged drug release with oral mucosa concentrations higher than its MIC of relevant pathogens.

Key words:
mucoadhesion –⁠ tablet –⁠ carbomer –⁠ controlled release –⁠ ciclopiroxolamine