Development of dexamethasone-loaded mixed polymeric micelles for nasal delivery

Eur J Pharm Sci. 2021 Nov 1:166:105960. doi: 10.1016/j.ejps.2021.105960. Epub 2021 Jul 31.

Abstract

Our study aimed to formulate a novel dexamethasone (DXM)-loaded, mixed polymeric micelle-based drug delivery system, focusing on the auspicious nose-to-brain pathway, as a key delivery route to treat central nervous system (CNS) associated diseases. Polymeric micelles might be a solution to deliver drugs to the place of action compared to conventional formulations. Due to low Z-average (89.92 ± 2.7 nm), a polydispersity index of 0.216 ± 0.014 and high surface polarity (52.23%), a significant increase in water solubility (14-fold) was experienced. This increase resulted in favourable dissolution profile at nasal and axonal conditions with high in vitro permeability value (14.6×10-6 cm/s) on polar brain (porcine) lipid extract. Modified Side-bi-side® type diffusion study confirmed rapid and efficient passive diffusion through the nasal mucosa contributed by strong mucoadhesive properties. The final formulation met all the requirements of a nasal drug delivery system with rapid onset of action, meaning DXM can reach the CNS and there it can exert its beneficial effects in pathological conditions.

Keywords: Binary system; Nasal formulation; Nose-to-brain delivery; Polymeric micelle; Solubility enhancement.

MeSH terms

  • Animals
  • Dexamethasone
  • Drug Carriers*
  • Drug Delivery Systems
  • Micelles*
  • Particle Size
  • Polymers
  • Solubility
  • Swine

Substances

  • Drug Carriers
  • Micelles
  • Polymers
  • Dexamethasone