Mucoadhesive Buccal Tablets Research Articles

Evaluation of a novel, natural oligosaccharide gum as a sustained-release and mucoadhesive component of calcitonin buccal tablets

The objective of this study was to evaluate the gum from Hakea gibbosa (hakea) as a sustained-release and mucoadhesive component in buccal tablets for a model peptide, namely, salmon calcitonin. Flat-faced core tablets containing either 12 or 32 mg of hakea and 40 µg (200 IU) of salmon calcitonin (sCT) per tablet were formulated using a direct compression technique and were coated with Cutina on all but one face. The in vitro release profiles were sigmoidal in nature and according to a mathematical model indicated super Case II transport as the primary mechanism of release. The resulting plasma sCT and calcium concentrations were determined following both intravenous administration and buccal application of mucoadhesive tablets in rabbits. Following intravenous administration, the mean values determined for t1/2 (α), t1/2 (β), Vd, and CL for sCT were 0.76 ± 0.06 min, 67 ± 18 min, 1484 ± 454 mL/kg, and 19 ± 2 mL/min·kg, respectively. Following the application of the mucoadhesive buccal tablets which contained 40 µg of sCT and either 12 or 32 mg of hakea, the calculated apparent bioavailability (F) and clearance (CL) were 37 ± 6% and 19 ± 3.3 mL/min·kg and 16 ± 8% and 18 ± 0.4 mL/min·kg, respectively. Serum calcium concentrations indicated that biologically active sCT was delivered across the rabbit buccal mucosa. The strength of mucoadhesion of the tablets was also quantitated in terms of the force of detachment as a function of time. The force of detachment for the mucoadhesive buccal tablets containing either 12 or 32 mg of hakea and 40 µg of sCT increased from 4.47 ± 0.68 to 8.41 ± 1.0 N and 8.23 ± 1.62 to 14.98 ± 1.63 N, respectively, from 5 to 90 min following application to excised rabbit intestinal mucosa. These results demonstrate that the novel, natural gum from Hakea gibbosa may be used to sustain the release of sCT from a unidirectional-release buccal tablet. The mechanism of in vitro release is likely to involve peptide diffusion/polymer dissolution. The mucoadhesive strength, as measured by the force of detachment, can be modulated by altering the amount of hakea in the tablet. The mucoadhesive buccal tablets described in this paper represent an improved transbuccal delivery system for therapeutic polypeptides.

Transmucosal sustained-delivery of chlorpheniramine maleate in rabbits using a novel, natural mucoadhesive gum as an excipient in buccal tablets

The objective of this study was to evaluate the gum from Hakea gibbosa (Hakea) as a sustained-release and mucoadhesive component in buccal tablets following their application to the buccal mucosa of rabbits. Flat-faced core tablets containing either 22 or 32 mg of Hakea and 40 or 25 mg of chlorpheniramine maleate (CPM) per tablet with either sodium bicarbonate or tartaric acid in a 1:1.5 molar ratio were formulated using a direct compression technique and were coated with Cutina® on all but one face. The resulting plasma CPM concentration versus time profiles were determined following buccal application of the tablets in rabbits. The strength of mucoadhesion of the tablets was also quantitated in terms of the force of detachment as a function of time. Following the application of the mucoadhesive buccal tablets, the following values for several pharmacokinetic parameters were obtained. The force of detachment for the mucoadhesive buccal tablets containing 22 mg of Hakea and either 25 and 40 mg CPM, and 32 mg Hakea and 40 mg CPM increased from 1.64±0.47 to 7.32±0.34 N, 1.67±0.30 to 7.21±0.36 N, and 2.93±0.73 to 7.92±0.60 N, respectively from 5 to 90 min following application to excised intestinal mucosa. Addition of either sodium bicarbonate or tartaric acid, as well as higher amounts of CPM, did not affect the mucoadhesive bond strength. These results demonstrate that the novel, natural gum, H. gibbosa, may not only be used to sustain the release of CPM from a unidirectional-release buccal tablet, but also demonstrate that the tablets are sufficiently mucoadhesive for clinical application. The mucoadhesive strength as measured by the force of detachment, can be modulated by altering the amount of Hakea in the tablet. The mucoadhesive buccal tablets evaluated represent an improved transbuccal delivery system for conventional drug substances.

Muco-adhesive Buccal Tablets of Clotrimazole for Oral Candidiasis

Muco-adhesive erodible buccal tablets of clotrimazole were formulated using a combination of bio-adhesive polymers like Carbopol-974P (CP-974P) and hydroxypropylmethylcellulose-K4M (HPMC-K4M), and soluble excipients like polyethylene glycol-6000 and mannitol. Increasing the concentration of CP-974P was found to increase the in vitro adhesion time as well as the bio-adhesive strength of the formulations. A combination of 7.5% of CP-974P and 42.5% of HPMC-K4M along with the soluble excipients in the erodible matrix, was found to release the drug for up to 3 hr, in vitro without getting dislodged. The drug released was found to be microbiologically active against Candida albicans. In vivo evaluation of the buccal tablet in healthy human volunteers and its comparison with a marketed troche formulation revealed that the muco-adhesive tablet produced more uniform and effective salivary drug levels with adequate comfort, taste, and non-irritancy over a period of 6 hr.

Interpolymer Complexation and its Effect on Bioadhesive Strength 6 Dissolution Characteristics of Buccal Drug Delivery Systems

AbstractDuring the process of development of mucoadhesive buccal delivery systems, interpolymer complex formation between carboxy vinyl polymer, which is similar to polyacrylic acid and other polymers as hydroxypropyl cellulose, carbopol-934, sodium carboxymethyl cellulose and polyvinyl pyrrolidone was studied as a function of pH. It was observed that carbopol-934 shows strong complexation with polyvinyl pyrrolidone and hydroxypropyl cellulose, but very little with sodium carboxymethyl cellulose. The degree of complexation is higher at acidic pH and decreases with an increase in pH. In further studies, when mucoadhesive buccal tablets were prepared using these polymer combinations, it was observed that the degree of complexation between the two polymers affected the rate and extent of drug release and also the bioadhesive strength of the tablets.