Conditions for attachment of ampicillin and gentamicin to nanoparticles were studied. A freeze-dried formulation was also developed. The release rate of ampicillin from nanoparticles was studied both with and without esterases. For polyisobutylcyanoacrylate nanoparticles, the liberation of the drug was enhanced in esterase-rich medium. By contrast, drug release as a consequence of enzymatic degradation of the polymer was not observed with polyisohexylcyanoacrylate nanoparticles. Finally, the antimicrobial activities of both ampicillin and gentamicin remained unaltered upon linkage of these molecules to the nanoparticles.