title: Polymeric mucoadhesive tablets for topical or systemic buccal delivery of clonazepam: Effect of cyclodextrin complexation.
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-βCD (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.
authors: Dept. of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
authors: P
authors: P
authors: Mura
authors: Dept. of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
authors: M
authors: M
authors: Cirri
authors: Dept. of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
authors: N
authors: N
authors: Mennini
authors: Dept. of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
authors: G
authors: G
authors: Casella
authors: Dept. of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy. Electronic address: francesca.maestrelli@unifi.it.
authors: F
authors: F
authors: Maestrelli
mesh_terms: D000269:Adhesives / Q000737:chemistry / Q000494:pharmacology; D000278:Administration, Buccal; D000287:Administration, Topical; D002998:Clonazepam / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D003505:Cyclodextrins / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D013607:Tablets
chemical_list: D000269:Adhesives; D003505:Cyclodextrins; D013607:Tablets; D002998:Clonazepam
keywords: Buccal delivery; Cyclodextrin; Polymeric tablet