Formulation and Optimization of Biodegradable Polylactic-coglycolic acid Nanoparticles of Simvastatin using Factorial design

The objective of the present work was to formulate nanoparticles for simvastatin drug. Simvastatin is a lipid lowering agent, 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, Pluronic F-68 as polymeric stabilizer. 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 % encapsulation efficiency, particle size, Polydispersity index, in vitro drug release pattern and drug excipient interactions. 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 formulation batch PS3 having lowest particle size 122 nm. 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.

Author(s): Anilkumar J. Shinde and Harinath N. More

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