Clarithromycin loaded lipid polymer hybrid nanoparticles: Fabrication, in vitro and in vivo evaluation

Abstract

Clarithromycin; a Macrolide antibiotic is used to treat various bacterial infections. Unluckily, its hydrophobic nature adds to its variable and pitiable oral bioavailability. In the current study, clarithromycin loaded Lipid Polymer Hybrid Nanoparticles (LPHNs) were produced followed by in vitro and in vivo evaluation. Clarithromycin loaded LPHNs (CHNF-5) with particle size 125.31±2.5nm and PDI (0.312±0.01) showed high entrapment efficiency 96%, and drug loading capacity 0.596 % ± 0.014. Spherical shaped particles were confirmed by scanning electronic microscopy. Differential Scanning Calorimetry and Powder X-Ray Diffraction confirmed the crystalline properties of the LPHNs. The engineered nanoparticles exhibited high stability at different temperature. Dissolution studies demonstrated that LPHNs effectively sustained the drug release rate. In vivo pharmacokinetic studies of the produced LPHNs demonstrated significant increase in the maximum peak plasma concentration (1390 ng/mL, P<0.001), AUC (14146 ng h/mL, P<0.001), and eradication half-life (11.6 h, P<0.01)