Development of Indomethacin Sustained Release Microcapsules using Ethyl Cellulose and Hydroxy Propyl Methyl Cellulose Phthalate by O/W Emulsification

Abstract

Indomethacin (IM) sustained release microcapsules were successfully prepared using ethyl cellulose (EC) and hydroxy propyl methyl cellulose phthalate (HPMCP) by o/w emulsification-solvent evaporation technique. The prepared microcapsules were evaluated for size, shape, drug content and in vitro drug release. The microcapsules show sustained release curves at pH 7.2 phosphate buffer for up to 6 h. The data obtained from the dissolution profiles were compared in the light of different kinetics models and the regression coefficients were compared. The in vitro dissolution study confirmed the Higuchi-order release pattern. Particle size and release data analysis from five consecutive batches prepared in the laboratory indicated suitable reproducibility of the solvent evaporation process. The release rate increased exponentially with the addition of HPMCP in EC. IM release rate was observed highest with the highest concentration of HPMCP (3:7 ratio of EC:HPMCP), used in the present studies. On the other hand, IM release rate was lowest when EC and HPMCP combination was used at the ratio of 10:0. When percent of HPMCP was increased, the particle size of microcapsules was decreased.

Application of Indomethacin in Medicine and Pharmacy

“…Microencap-sulation of indomethacin into biodegradable particles of polylactide-glycolide and its copolymer polylactide-polyethelene glycole using compressed CO 2 allowed getting sustained release of the model drug [10]. Desired compositions of indomethacin sustained release microcapsules using ethyl cellulose, hydroxy propyl methyl cellulose, and chitosan-carboxymethyl-cellulose are described [11].…”

Ultrasonic atomization and polyelectrolyte complexation to produce gastroresistant shell–core microparticles

“…It can also have chemoprotective effects against tumors, reducing the risk of colon cancer . It has poor water solubility, a short biological half‐life of about 2.6–11.2 hours with an usual oral dosage (the administration route with highest patient compliance) for adults of 25 or 50 mg, for two to three times a day . Indomethacin has physical properties which may cause severe side effects on the gastrointestinal tract, such as stomach irritation, intestinal bleeding or ulcers, and can increase blood pressure and decrease kidney function…”

“…Electrospraying process was successfully used to prepare indomethacin‐loaded microparticles of inuline acetate, a natural polysaccharide . Indomethacin sustained release microcapsules were prepared by solvent evaporation from an oil (O)/water (W) emulsion using ethyl cellulose and hydroxy propyl methyl cellulose phthalate (release retardants) . The pH‐sensitive Eudragit L‐100 microspheres containing indomethacin and encapsulating magnetic nanoparticles were prepared by a solvent evaporation method for biomedical, tissue engineering, and magnetic resonance applications .…”