Anilkumar J. Shinde, Harinath N. More
The objective of the present work was to formulate nanoparticles for simvastatin drug. Simvastatin is a lipid lowering agent, and BCS class-II drug having low solubility and high permeability. Since simvastatin undergoes extensive first pass extraction in the liver, the availability of the drug to the general circulation is low (< 5%). Nanoparticles were prepared by precipitation-solvent deposition method using 3² full factorial design. From the preliminary trials, the constraints for independent variables X1 (amount of PLGA) and X2 (amount of Pleuronic F-68) have been fixed. The prepared formulations were further evaluated for drug content, in vitro drug release pattern, short term stability and drug excipient interactions. The application of factorial design gave a statistically systematic approach for the formulation and optimization of nanoparticles with desired particle size and high entrapment efficiency. Drug: polymer ratio and concentration of stabilizer were found to influence the particle size and entrapment efficiency of simvastatin loaded PLGA nanoparticles. In vitro drug release study of selected factorial formulations (PS1, PS4, PS7) showed, 84.56%, 89.65 %, and 73.46 % release respectively in 24 hrs. The release was found to follow first order release kinetics with fickian diffusion mechanism for all batches. These results indicate that simvastatin loaded PLGA nanoparticles could be effective in sustaining drug release for a prolonged period.
