Release of indomethacin from pH-sensitive pullulan acetate microsphere

Abstract

We studied the pH-sensitive indomethacin (IND) delivery system using pullulan. Hydrophobic pullulan acetate was prepared by chemical modification of hydrophilic pullulan and pullulan acetate microsphere was made by a solvent evaporation method. The size of microspheres was below 5 μm, and the drug loading efficiencies of microspheres were approximately 78 and 65% at the initial amount of drug 40 and 80 mg, respectively. The microsphere showed pH-sensitive swelling behavior in PBS buffer. After 15 hrs, the swelling of the microsphere at pH 7.4 was approximately 20 times greater than that at pH1.2. The pH of the medium significantly influenced on thein vitro release rate. The released amount of drug at pH 7.2 was approximately 90 times greater than that at pH 1.2. The shape of microspheres at pH 1.2 were maintained sphere forms, but at pH 7.4 were disintegrated. The pH-sensitive IND release pattern was due both to the pH-sensitive diffusion of IND from the microspheres and to the release of the drug from the surface which underwent disintegration after swelling, due to the chemical composition of the microspheres and the pH of the release media.