Polymeric mucoadhesive tablets for topical or systemic buccal delivery of clonazepam: Effect of cyclodextrin complexation.
Two kinds of mucoadhesive buccal tablets of clonazepam (CLZ) were developed to provide, a prolonged local or systemic delivery respectively. Tablets prepared by direct compression of combinations of different polymers were tested for swelling, erosion and residence time properties. Carbopol 971P/hydroxypropylmethylcellulose and Poloxamer/chitosan mixtures were the best and were selected for drug loading. The effect of CLZ complexation with different cyclodextrins was investigated. Randomly methylated bCD (RAMEssCD) was the most effective, allowing 100% drug released increase from local delivery buccal tablets. Kollicoat was the best among the tested backing layers, assuring a unidirectional release from systemic delivery buccal tablets <0.8% drug released in simulated saliva after 24h) In vitro permeation studies from coated tablets showed that CLZ loading as RAMEssCD coground enabled a 5 times increase in drug flux and permeability. Therefore, complexation with RAMEssCD was a successful strategy to improve the CLZ performance from buccal tablets for both local or systemic action.
Carbohydrate polymers