Hollow pessary loaded with lawsone via self microemulsifying drug delivery system for vaginal candidiasis
Abstract An attempt was made to enhance solubility of an antifungal agent lawsone, via self microemulsifying drug delivery system (SMEDDS) formulated further into hollow pessary to treat vaginal candidiasis. Microemulsion was formed at 20% capryol 90(r) (oil) 80% Gelucire 44/14(r) (surfactant) and 20% Tween 80 (co surfactant) which was plotted using pseudo ternary phase diagram using aqueous titration method. Zeta potential 10.9 0.54 mV and particle size 12.19 1.13 nm confirmed the formation of microemulsion. Quick self emulsification time (55 s) indicated rapid emulsification process at vaginal site. Cloud point confirmed the stability of SMEDDS (up to 60 degC) Lawsone loaded SMEDDS exhibited improved solubility of lawsone (216 2.54 mg/ml and 0.542 0.04 mg/ml, respectively) and dissolution, which further helped to enhance its antifungal activity. Pessary base, consisted of Ovucire WL3460(r) (94, 96, 98) and beeswax (2, 4, 6) was optimized using three level, two factor full factorial design. Hollow pessary was further fabricated using melted base (at 60 degC) which was poured into aluminum mold fitted with center tube. This center tube was filled with lawsone loaded SMEDDS and was solidified at 2 8 degC. Pessary was melted within 7 1.1 min at 37 degC and released 96.96 1.43% lawsone within 1 h at simulated vaginal fluid. Lawsone SMEDDS loaded pessary released lawsone at par with marketed clotrimazole vaginal tablet. To conclude, hollow pessary of lawsone loaded SMEDDS can be an advanced modality to treat vulvo vaginal candidiasis.