Abstract

DEVELOPMENT AND CHARACTERIZATION OF LOVASTATIN LOADED POLYMERIC NANOPARTICLES FOR THE TREATMENT OF HYPERLIPIDEMIA

Soyab Patel* and Shakeel Memon

ABSTRACT

An attempt was made to prepare polymethylmethaacrylate based synthetic nanoparticles loaded with lovastatin for improved treatment of hyperlipidemia. The nanoparticles were characterized by transmission electron microscopy, particle size, zeta potential, entrapment efficiency, FTIR, differential scanning calorimetry and x-ray diffraction analyses. The in-vitro drug release and in vivo hyperlipidemia activity was also performed. The prepared nanoparticles were spherical with some looser aggregates. The size was in the range of 195.4 to 752.9 nm and zeta potential in the range of -1.13 to -3.26 mV. The DEE was found to be in the range of 44.36% to 59.45%. As the concentration of polymer was increased in the nanoparticles, the DEE was decreased. The DSC and XRD analyses indicated the amorphous dispersion of drug in the nanoparticles. FTIR study indicated the stability of lovastatin within the nanoaprticles. The in vitro drug release indicated that the drug release was continued up to 24 hrs; that as the concentration of polymer was increased, the drug release rate was decreased and on the other hand, as the as the amount of lovastatin was increased the drug release was increased. Drug release mechanism followed non-Fickian transport. The hypolipidemic activity performed on Wistar rats indicated that the prepared nanoparticles have reduced the total cholesterol and triglycerides in the blood plasma. This indicates that the nanoparticles were capable of releasing the lovastatin for prolonged period to maintain the constant plasma drug concentration.

Keywords: Polymeric Nanoparticle, Polymethylmethaacylate, DSC, XRD, DEE, In vivo study.