Double-tailed acyl glycoside niosomal nanocarrier for enhanced oral bioavailability of Cefixime

Artif Cells Nanomed Biotechnol. 2017 Nov;45(7):1440-1451. doi: 10.1080/21691401.2016.1246451. Epub 2016 Nov 8.

Abstract

Novel, safe, efficient, and cost effective surfactants from renewable resources has attracted attention for enhancing solubility and bioavailability of hydrophobic dugs. We report the synthesis, characterization, and biocompatibility of a novel non-ionic acyl glycoside double-tailed surfactant for niosomal drug delivery system. Structure of the surfactant was confirmed by 1H NMR and mass spectroscopy. Applications of surfactant in niosomal drug delivery were explored using Cefixime as model. The shape, size, and polydispersity index (PDI) of drug loaded vesicles were investigated with atomic force microscope (AFM) and dynamic light scattering (DLS). Drug entrapping efficiency (EE%) was determined using HPLC. Biocompatibility of the surfactant was evaluated by in vitro cytotoxicity, blood hemolysis, and in vivo acute toxicity. Bioavailability of the surfactant based formulation was investigated in rabbits using HPLC. Vesicles were found to be 159.76 ± 6.54 nm with narrow size distribution and spherical shape. EE% was found to be 71.39 ± 3.52%. Novel surfactant was non-cytotoxicity and hemo-compatible even at 1000 μg/mL concentration and was safe up to 2000 mg/kg body weight. The in vivo bioavailability of niosomal formulation showed elevated plasma concentration and decreased clearance of Cefixime. Current findings reveal that this novel surfactant is biocompatible and could be employed for niosomal drug delivery.

Keywords: Cefixime; Nonionic surfactant; bioavailability; biocompatibility; synthesis.

MeSH terms

  • Animals
  • Biological Availability
  • Cefixime / administration & dosage*
  • Cefixime / chemistry
  • Cefixime / pharmacokinetics*
  • Drug Carriers / chemistry*
  • Drug Carriers / toxicity
  • Drug Liberation
  • Female
  • Glycosides / chemistry*
  • Hemolysis / drug effects
  • Humans
  • Liposomes / chemistry*
  • Liposomes / toxicity
  • Male
  • Materials Testing
  • Mice
  • Rabbits

Substances

  • Drug Carriers
  • Glycosides
  • Liposomes
  • Cefixime