CIPROFLOXACIN-LOADED POLYISOBUTYLCYANOACRYLATE NANOPARTICLES - PHARMACOKINETICS AND IN-VITRO ANTIMICROBIAL ACTIVITY

The disposition of ciprofloxacin in free form and loaded PIBCA/NP has been studied after intravenous infusion to the rabbit. Data from plasm a concentration profiles revealed that pharmacokinetic parameters of c iprofloxacin associated with the colloidal carrier were greatly modifi ed. Thus, ciprofloxacin-loaded PIBCA/NP led to increased AUG, t(1/2) a nd V-d, and to a decreased Cl as compared with drug in solution. This could be due not only to the colloidal drug carrier but also to the ph armacokinetics of ciprofloxacin itself. Studies of efficacy against My cobacterium? avium complex in human macrophages proved that ciprofloxa cin-loaded PIBCA/NP was more effective than free drug. The cytotoxicit y of the polymeric material was observed at concentrations higher than 80 mu g of PIBCA per mi with drastic reduction of viable macrophages. This may explain why the efficacy of ciprofloxacin associated with na noparticles was much lower than expected. (C) 1998 Elsevier Science B. V. All rights reserved.