TOLMETIN POLY-D,L-LACTIDE MICROSPHERES - IN-VITRO IN-VIVO EVALUATION

Poly-D,L-lactide microspheres loaded with a non-steroidal anti-inflammatory drug (tolmetin) were prepared. The purpose the paper is the in vitro/in vivo evaluation of a microparticulate drug delivery system containing tolmetin and intended br parenteral administration. Microsphere preparation was carried out by two different techniques : emulsification solvent evaporation and spray drying. Each method involves different process variables that were experimentally assessed. Spherical shaped particles whose size varied between 3.5 and 7.5 mu m, whose drug content was between 4.5 and 9.5%, were obtained. In vitro drug release from microspheres was tested by he rotating paddle method(FUIIX Ed.). Biological evaluation hows the suitability of a microparticulate system for chronic administration of tolmetin. The anti-inflammatory effect of tolmetin-loaded microspheres, rested in vivo on models of and chronic inflammation, was comparable to the effect of the free drug but significantly sustained.