Preparation and physicochemical evaluation of indomethacin sustained-release microspheres for ophthalmic delivery / 中国药学杂志

ABSTRACT

OBJECTIVE: To obtain sustained-release indomethacin PLGA/Eudragit RS 100 microspheres for ophthalmic application and to evaluate its quality. METHODS: The microspheres were prepared by O/W solvent evaporation using PLGA and Eudragit RS 100. The morphological, drug content, entrapment efficiency, release behavior, particle size, residual organic solvent, Zeta potential of indomethacin PLGA/Eudragit RS 100 microspheres were determined; meanwhile, the cytotoxicity of blank microspheres was evaluated using PRE cells. RESULTS: Indomethacin microspheres containing PLGA and Eudragit RS 100 at the weight ratio of 1 3 had even particle size distribution, and their surfaces were smooth under scan electronic microscope; and the mean diameters were (1676.4 ± 739.5) nm. The drug content and entrapment efficiency of the microspheres were (18.79 ± 0.19)% and (98.25 ± 2.11)%, respectively. Indomethacin was released slowly for a month from the microspheres, though burst release was observed within 24 h. The mean residual organic solvent was (267.33 ± 13.57) ppm. The zeta potential of all blank PLGA / Eudragit RS 100 microspheres was positive. The blank microspheres showed no sign of toxicity. CONCLUSION: Indomethacin PLGA / Eudragit RS 100 microspheres have a better clinical application prospect due to its high entrapment efficiency, narrow distribution, slow release and ocular safety. Copyright 2012 by the Chinese Pharmaceutical Association.