NANOPARTICULATE DRUG DELIVERY SYSTEM OF CYCLOSPORINE

Recent research on idealizing drug delivery systems which is progressing at a prodigious rate, aims at the development of drug delivery systems with maximum therapeutic benefits of drug delivery thus resulting in safe and effective management of diseases. In the present study Nanoparticlulate drug delivery system for Cyclosporine was developed, that would overcome the therapeutic risks of conventional formulations and was evaluated with respect to particle size, drug content, in vitro release and in vivo targeting. Cyclosporine is a first line immunosuppressive drug used to prevent transplant rejection and in treatment of autoimmune diseases. The commercially available formulations of Cyclosporine are associated with acute hemodynamic changes that result in nephrotoxicity and also have low bioavailability. Cyclosporine (CYA) loaded Eudragit RL100 nanoparticles were prepared using solvent evaporation technique, with 2% PVA as stabilizer. Four batches of nanoparticles with varying drug concentrations (CYN-1, CYN-2, CYN-3 and CYN-4) were prepared. Cumulative % drug release of formulations CYN-1, CYN-2, CYN-3 and CYN-4 was 94.35%, 93.89%, 88.28% and 85.36% respectively. Formulation CYN-2, which proved to be the best showed a mean particle size of 236 nm and entrapment efficiency of 58.27%. The in vivo result of formulation CYN-2 revealed that the drug loaded nanoparticles showed preferential drug targeting to liver followed by spleen, lungs and kidneys. Stability studies showed that maximum drug content and closest in vitro release to initial data was found in the sample (formulation CYN-2) stored at 4C. So, in the present study Cyclosporine loaded Eudragit Nanoparticles were prepared and targeted to various organs to a satisfactory level and the prepared nanoparticles were stable at 4C.