A smart gelatin nanoparticle for delivery of metoprolol succinate: A strategy for enhancing the therapeutic efficacy by improving bioavailability

Abstract

The purpose of this study was to develop and evaluate of gelatin nanoparticles (GNPs) by nanoprecipitation method to increase metoprolol succinate (MES) peroral bioavailability. Prepared GNPs were evaluated in terms of its properties such as particle size, zeta potential, entrapment efficiency, drug loading, in vitro drug release, morphologyand in-vivo pharmacokinetic studies. The GNPs showed sustain drug release in phosphate buffer (pH 7.4) while less release in the 0.1 N HCl as compared to plain MES. The in vivo pharmacokinetics study on rabbits showed a rise in the bioavailability of the GNPs by 2.27 folds as compared to marketed formulation. FTIR studies performed on the GNPs indicated no drug-polymer interaction. Nanoparticles (NPs) prepared by nanoprecipitation method were found to be clear (through SEM) and their mean particle size was in the range of 59.83±0.14 to156.41±0.19 nm. The F-3 formulation exhibited the highest entrapment of 98.07±0.53. Zeta potential of all GNPs was in the range of 11.66 to 14.50 mV which indicates that they are moderately stable. Release study revealed that GNPs release drug at a sustained rate which assists in the absorption of MES through the blood. Further, in vivo studies induced in increased bioavailability of the MES which established the potential of developed carrier systems. Thus, it can be concluded that these prepared NPs might be one of the best preparation for the delivery of MES for better therapeutic efficacy.