DESIGN, DEVELOPMENT, PHYSICOCHEMICAL CHARACTERISATIONS AND IN VITRO EVALUATION OF KETOPROFEN MICROSPHERES


Varshney H.M., Tanwar Y.S., Chauhan B.S., Sharma P.K.

ABSTRACT
Background and the purpose of the study: Generally, drug release from biodegradable polymer depends upon the drug solubility in the polymer, the chemical composition of the polymer and drug particle size. Ketoprofen exhibits short half-life, poor compressibility, caking tendency, gastrointestinal irritation & ulcerogenic effect. Hence, it is desirable to formulate into sustained release dosage form. Microspheres of ketoprofen were developed as oral sustained release dosage form using ethyl cellulose as the coating/ matrix forming material or release retarding material, influence of non-solvent used for the polymer solution i.e. acetone and dichloromethane, employed in the formulation was studied on the drug release from ethyl cellulose microspheres.
Methods: Ketoprofen microspheres were formed using solvent evaporation technique in different ratios and by using different stirrer speed. The microspheres were evaluated for size distribution, surface characteristics, drug content, drug entrapment efficiency, drug release characteristics.
Results and major conclusion: The use of different ratio of ethyl cellulose polymer, different mixing amount of solvent ratio and different stirring speed clearly indicates that the formulations can delay the drug release prior to microspheres. The maximum release of the ketoprofen microsphere was found with FM-3, they can be arranged as increasing order- FM-3 > FM-4 >FM-5 > FM-2 > FM-1. Poorly water soluble ketoprofen loaded microspheres safely improve the solubility and/or absorbability of drug.
Keywords: Ketoprofen, Ethyl cellulose, Acetone, Dichloromethane