Formulation and physicochemical characterisation of buccoadhesive films containing ketorolac

Abstract

Ketorolac tromethamine, the non-steroidal anti-inflammatory drug, was formulated onto buccoadhesive films to overcome the limitations in the currently available dosage and routes of administration which in sequence will increase patients’ compliance. Films were cast from organic and aqueous solvents using various bioadhesive polymers namely: sodium carboxymethyl cellulose (Na-CMC), hydroxypropyl cellulose (HPC), hydroxypropylmethyl cellulose (HPMC) and Carbopol 934. The prepared films were subjected to investigations for their physical and mechanical properties, swelling behaviors, in vitro bioadhesion, drug permeation via bovine buccal mucosa and in vitro drug release. These properties were found to vary significantly depending on the preparation methods, the type of the polymers and the ratio of addition of both plasticizer (i.e. polyethylene glycol) and film forming agent (ethyl cellulose and polyvinylpyrolidene). Formula number K10 containing carbopol 0.5% and HPMC 0.5% was found to be the best film as it shows good adhesion, acceptable pH, and gives a reasonable ketrolac release (about 85-90% at 6h). In addition, this film was subjected to in vitro and in vivo release. The obtained results indicate that the concentration of ketorolac in the oral cavity was maintained above 4.0μg/mL for a period of at least 6h. This film shows promising results for using the ketrolac buccoadhesive route of administration topically and systemically, and thus it will be subjected to clinical evaluation in future work.