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-beta CD (RAME beta CD) 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 24 h). In vitro permeation studies from coated-tablets showed that CLZ loading as RAME beta CD-coground enabled a 5-times increase in drug flux and permeability. Therefore, complexation with RAME beta CD was a successful strategy to improve the CLZ performance from buccal tablets for both local or systemic action.

Polymeric mucoadhesive tablets for topical or systemic buccal delivery of clonazepam: Effect of cyclodextrin complexation / Mura, P.; Cirri, M.; Mennini, N.; Casella, G.; Maestrelli, F. - In: CARBOHYDRATE POLYMERS. - ISSN 0144-8617. - ELETTRONICO. - 152:(2016), pp. 755-763. [10.1016/j.carbpol.2016.07.075]

Polymeric mucoadhesive tablets for topical or systemic buccal delivery of clonazepam: Effect of cyclodextrin complexation

MURA, PAOLA ANGELA;CIRRI, MARZIA;MENNINI, NATASCIA;CASELLA, GIADA;MAESTRELLI, FRANCESCA
2016

Abstract

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-beta CD (RAME beta CD) 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 24 h). In vitro permeation studies from coated-tablets showed that CLZ loading as RAME beta CD-coground enabled a 5-times increase in drug flux and permeability. Therefore, complexation with RAME beta CD was a successful strategy to improve the CLZ performance from buccal tablets for both local or systemic action.
2016
152
755
763
Mura, P.; Cirri, M.; Mennini, N.; Casella, G.; Maestrelli, F
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1080086
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