ABSTRACT:
The goal of the present investigation was to formulate and evaluate a potential of chitosan nanoparticles as carriers for the lovastatin drug. Lovastatin is a BCS class-II drugs having low solubility and high permeability. Since lovastatin undergoes extensive first pass extraction in the liver, the availability of the drug to the general circulation is low (< 5%). Nanoparticles were prepared by modified ionotropic gelation method using 3² full factorial design. From the preliminary trials, the constraints for independent variables X1 (concentration of chitosan) and X2 (concentration of sodium tripolyphosphate) have been fixed. Factors included concentration of chitosan and STPP, have been examined to investigate effect on particle size, encapsulation efficiency, zeta potential, % release, SEM, FTIR, XRD and DSC analysis of lovastatin. Release study was conducted by in vitro dialysis membrane method using phosphate buffer pH 7.4 at 37oC. The diameter of prepared nanoparticles was controlled in the range of 100 - 800nm. Experimental results showed that lovastatin encapsulation efficiency was decreasing with increasing chitosan concentration. The particle size is independent of encapsulation efficiency. Spectrograms of FTIR and DSC showed that lovastatin physically absorbed by chitosan matrix. SEM photographs demonstrated prepared nanoparticles were in spherical shape and narrow diameter distribution. In vitro drug release study of selected factorial formulations (CL1, CL4, CL7) showed, 87.42± 0.020 %, 85.72± 0.025%, and 78.88± 0.025% release respectively in 24 hrs. The Zeta potential of all the batches were in the range of + 30 mv and batch CL4 was found to be + 35.32 mv. So it conclude that prepared all formulation were good stability. The release profiles of all batches were very well fitted by both the zero order mode and the anomalous transport. These results indicate that lovastatin nanoparticles could be effective in sustaining drug release for a prolonged period.