Nanosuspensions by Solid Lipid Nanoparticles method for the Formulation and In vitro/in vivo, characterization of Nifedipine

Abstract

Nifedipine is a dihydropyridine calcium channel antagonist initially prescribed for treatment of angina pectoris and hypertension. The drug belongs to BCS Class-2 drug, is poorly water soluble drug, it suffers from a poor aqueous solubility, hence the delays its onset of action. Therefore, the purpose of the research study is to adopt the nanotechnology to formulate nanoparticles that improve the rate of dissolution of drug and to get desired bioavailability of nifedipine. Nanosuspensions were prepared by Solid Lipid Nano Particles method in the presence of selected stabilizers at different concentrations. The nanosuspensions were determined for their particle size of drug, zeta potential of drug, drug content and drug dissolution. The selected formula was freeze dried and illustrated by scanning electron microscopy (SEM), FT-IR, differential scanning calorimetry (DSC), and pharmacokinetic study. The in vitro dissolution confirmed the rate of drug release greater compared to the pure drug. The optimum formula has a typical particle size of 225.56±4.65nm and zeta potential of -17.84±2.17 mV. The bioavailability parameters in the rabbits were enhanced by 2 folds when compared with the marketed tablets (Calcigard®). Solid lipid nanoparticles method was successfully employed to produce stable Nifedipine nanosuspension by using the suitable concentration of stabilizer (PVA, Tween 80, PVP and HPMC). From this study, it is concluded that formulation of Nifedipine nanosuspension may be a competent approach that boost the rate of dissolution and hence oral bioavailability of drug.