Cyclodextrin complexation highly enhances efficacy of arylsulfonylureido benzenesulfonamide carbonic anhydrase inhibitors as a topical antiglaucoma agents

Two new sulfonamides incorporating arylsulfonylureido moieties were complexed with gamma cyclodextrin (c-CD), hydroxypropyl-gamma cyclodextrin (HPc-CD), hydroxypropyl-beta cyclodextrin (HPb-CD) and hydroxyethyl-beta cyclodextrin (HEb-CD) in order to obtain drug formulations with effec- tive topical intraocular pressure (IOP) lowering effects, in an animal model of glaucoma. The HPc-CD was the best solubilizing agent for the two sulfonamides and its complexes were characterized in detail and administered to rabbits with eye hypertension of 45–50 mm Hg. The peak IOP lowering was observed after 1 h post-administration and was of 36–37 mm Hg. A low IOP pressure (of around—35 mm Hg) was then maintained for the next 24 h post-administration, which has not been observed before with any IOP lowering drug