Formulation and evaluation of self-microemulsifying drug delivery system of lovastatin

Purpose: Lovastatin is poorly water soluble drug. It should be come into the BCS II drug. So oral bioavailability of lovastatin is less (50%). To develop novel dosage foam of the self-microemulsifying drug delivery systems (SMEDDS) for the lovastatin. Methods: Before the formulation of SMEDDS, solubility study was performed in different exicipients and select exicipients on basis of solubility of lovastatin. Microemulsion region was decided by preparing ternary phase diagram. Drug exicipients interaction study performed using DSC and FTIR. After preliminary study, SMEDDS formulations were prepared in sunflower oil (oil), Acrysol K140 (surfactant), Capmul MCM C8 (co-surfactant) and PEG400 (co-solvent) by simple mixing at 40 ̊C. Parameters evaluated included: macroscopic evaluation, visual assessments, self emulsification, transmittance test, droplet size, zeta potential and stability study, In vitro dissolution. Droplet size after incubation in simulated gastric fluid (SGF) or simulated intestinal fluid (SIF) via dynamic light scattering. In vitro dissolution was carried in USP apparatus II using 0.1 mol/l HCl at 50 r/min. Drug release was measured by spectroscopic method. Results: from the solubility study, better solubility was seen in sunflower oil (oil), Acrysol K140 (surfactant), Capmul MCM C8 (co-surfactant). No any drug exicipients interaction was seen. Droplet size was 18 to 24 nm. Formulation was clear and near to 100% transmittance after dilution with 0.1 mol/l HCl and Water. Drug was release up to 92 % in 1 h. Release data was compare with marketed product and calculate the f2 value and P value. f2 value was 12.19 and 13.15 that value was near to 0 and P value was less than 0.005. Conclusion: SMEDDS lovastatin oral formulations were prepared that provide excellent drug solubilization, drug stability in water and 0.1 mol/l HCl and improved in vitro release of lovastatin compare to marked product.