Development and in vitro evaluation of buccoadhesive carvedilol tablets

Abstract

Buccal delivery of drugs provides an attractive alternative to the oral route of drug administration, particularly in overcoming deficiencies associated with the latter mode of administration. Problems such as high first-pass metabolism and drug degradation in the harsh gastrointestinal environment can be circumvented by administering the drug via the buccal route (1-3). Moreover, buccal drug absorption can be promptly terminated in case of toxicity by removing the dosage form from the buccal cavity. It is also possible to administer drugs to patients who cannot be dosed orally to prevent accidental swallowing. Therefore adhesive mucosal dosage forms were suggested for oral delivery, which included adhesive tablets (4-6), adhesive gels (7, 8) and adhesive patches (9, 10). Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were composed of HPMC K4M or HPMC K15M in ratios of 1:1 to 1:5 whereas in the BE series Carbopol 934 was used (1:0.25 to 1:1.50). The formulations were tested for in vitro drug release, in vitro bioadhesion, moisture absorption and in vitro drug permeation through porcine buccal mucosa. Formulation BC3 showed maximum release of the drug (88.7 ± 0.4%) with the Higuchi model release profile and permeated 21.5 ± 2.9% of the drug (flux 8.35 ± 0.291 µg h -1 cm -2 ) permeation coefficient 1.34 ± 0.05 cm h -1 ) through porcine buccal membrane. BC3 formulation showed 1.62 ± 0.15 N of peak detachment force and 0.24 ± 0.11 mJ of work of adhesion. FTIR results showed no evidence of interaction between the drug and polymers. XRD study revealed that the drug is in crystalline form in the polymer matrix. The results indicate that suitable bioadhesive buccal tablets with desired permeability could be prepared.

A clinical perspective on mucoadhesive buccal drug delivery systems

“…Studies revealed that increasing the concentration of the polymer in the formulations showed a sustained effect on carvedilol release. The rapidly hydrating polymer dominated in controlling the release of carvedilol from the buccal tablets[31]. Propranolol hydrochloride (PRO-HCl), a nonselective beta-adrenergic blocking agent, has been widely used in the treatment of hypertension, angina pectoris, and many other cardiovascular disorders.…”

Development of Bio-adhesive Buccal Tablet of Nicorandil Using Factorial Approach

“…Moreover, such type of delivery is considered to be safer since any time, drug absorption can be concluded if any toxicity occurs due to it by removing the formulation from the site of application. [12][13][14] . Thus, in the present research paper, buccal bio-adhesive tablet of nicorandil was prepared using a sustainedrelease polymer HPMC K100M 10,15 , bio-adhesive polymer neem gum 16 and an impermeable backing layer of ethyl cellulose.…”

Development of amitriptyline buccoadhesive tablets for management of pain in dental procedures

“…These bioadhesive polymers could also resist salivation, tongue movement, and swallowing for a significant period of time 29 . HPMC has been applied to formulate buccoadhesives of drugs like metronidazole, benzydamine, carvedilol, and so on 21,26 . The buccoadhesives of some drugs like metronidazole, benzydamine, prednisolone, and pindolol have been prepared by means of NaCMC as well 26,30,31 .…”

“…Among the various transmucosal routes, buccal mucosa has excellent accessibility that offers painless administration, easy drug withdrawal, fast onset of action, patient compliance, and attractive alternative for noninvasive delivery of some drugs [13][14][15][16][17][18][19][20] . The buccal region of the oral cavity is an attractive target for administration of the drug of choice 21 . Local delivery in the oral cavity has had particular applications in the treatment of toothache, periodontal diseases, and bacterial infections 22 such as toothpastes, mouthwashes, lozenges, gels, chewing gums, lollipops, films, patches, and tablets have developed for topical oral administration 19,23 .…”