Glibenclamide nanosuspension inhaler: development, in vitro and in vivo assessment

Drug Dev Ind Pharm. 2020 May;46(5):762-774. doi: 10.1080/03639045.2020.1753062. Epub 2020 Apr 20.

Abstract

Objective: The development of nanosuspension for targeted delivery of glibenclamide as hypoglycemic agent to the lung in an inhaler dosage form.Method: Glibenclamide nanosuspension formulations were prepared using Box-Behnken design to investigate the effect of independent factors on the dependent variables, Fourier-transform Infrared spectroscopy, Differential Scanning Calorimetry, evaluation of glibenclamide nanosuspension inhaler and in vivo hypoglycemic efficacy were performed to determine glibenclamide nanosuspension inhaler effect.Results: The results revealed that the mean particle sizes of the prepared nanosuspension ranged from 0.216 to 0.856 µm, zeta potential from +9 to +16 mV, the solubility ranged from 43% to 75%, the mass median aerodynamic diameter was 2.34 µm and the glucose level in rat was significantly reduced by about 60%.Conclusion: These results confirmed that glibenclamide nanosuspension inhaler enhance hypoglycemic effectiveness and reduce adverse effect of glibenclamide, opening up new dosage form in Diabetes mellitus treatment.

Keywords: Diabetes mellitus; glibenclamide; inhaler; nanosuspension; optimization.

MeSH terms

  • Animals
  • Blood Glucose / drug effects
  • Blood Glucose / metabolism
  • Diabetes Mellitus, Experimental / drug therapy*
  • Diabetes Mellitus, Experimental / metabolism
  • Drug Development / methods*
  • Glyburide / administration & dosage
  • Glyburide / chemistry*
  • Glyburide / metabolism
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / metabolism
  • Male
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Nanoparticles / metabolism
  • Nanotechnology / methods
  • Nebulizers and Vaporizers*
  • Particle Size
  • Rats

Substances

  • Blood Glucose
  • Hypoglycemic Agents
  • Glyburide