Effect of adding non-volatile oil as a core material for the floating microspheres prepared by emulsion solvent diffusion method

Abstract

Eudragit(R) microspheres, to float in the gastrointestinal tract, were prepared to prolong a gastrointestinal transit time. To enhance their buoyancy, non-volatile oil was added to the dispersed phase. When an oil component was not miscible with water, over 90% was entrapped within the microspheres and prolonged the floating time of the microspheres. Depending on the solvent ratio, the morphologies of the microspheres were different and the best result was obtained when the ratio of dichloromethane: ethanol: isopropanol was 5:6:4. As the isopropanol portion increased, the time to form microspheres was delayed and the amount of fibre-like substance produced was decreased, due to the slow diffusion rate of the solvent. Compared with microspheres prepared without non-volatile oil, the release rate of the drug from microspheres was faster in all cases tested, except the microspheres containing mineral oil. The solubility of the drug in the non-volatile oil affected the release profiles of the drugs. The non-volatile oil tends to decrease the glass transition temperature of prepared microspheres and change the release profile. The internal morphology of the microspheres was slightly different depending on the entrapped oil phase used. Tiny spherical objects were present at the inner surface of microspheres and the inside of the shell.