Formulation and Characterization of Ciclopirox Olamine Mucoadhesive Effervescent Tablets for Vaginal Delivery

Abstract

The study was aimed to design and evaluate a new effervescent mucoadhesive vaginal drug delivery system for ciclopirox olamine (CPO), a broad-spectrum antifungal, antibacterial, and anti-inflammatory agent for effective treatment in vaginal candidiosis. Various polymers like Polyox 303, Carbopol 974P, HPMC K4M, Sodium CMC, HPC, Sodium Alginate, Xanthan Gum, Polycarbophil and Chitosan were used in the formulation of CPO effervescent mucoadhesive vaginal tablet (EMVT) employing direct compression as a method of preparation. The effervescent mixture (citric acid and sodium bicarbonate) was incorporated into the formulations to aid quick wetting and mucoadhesion of tablet followed by drug release modulation. The amount of polymer blends and effervescent mixture was optimized using 32 full factorial design. The swelling, mucoadhesive strength and in-vitro release were studied as dependent responses. The ex-vivo mucoadhesion was determined by modified mucoadhesion assembly. The ex-vivo residence test was carried out by modified USP dissolution test apparatus. In vitro anti-fungal activity of the CPO EMVT was determined in comparison to Candid®-V3 tablet. A good sustained effect and a moderate mucoadhesion (0.31N to 0.67N) were obtained with tablets containing HPMC K4M: Polyox 303 (1:1.4) and effervescent mixture (1:3). Ex-vivo mucoadhesion time of all the formulations was in the range of 8 to 24 h. The effervescent CPO tablet showed significantly higher in-vitro antifungal activity as compare to Candid®-V3 tablet (p< 0.05). The results of short term stability revealed stable characteristics of optimized formulation. The proposed formulation may provide a potential antifungal activity against Candida albicans.