Impact of physicochemical properties of nasal spray products on drug deposition and transport in the pediatric nasal cavity model

Int J Pharm. 2020 Jan 25:574:118911. doi: 10.1016/j.ijpharm.2019.118911. Epub 2019 Dec 3.

Abstract

The study is focused on the analysis of physicochemical properties of selected nasal sprays of mometasone furoate, and the influence of these properties on aerosol quality and penetration in the pediatric nose. After the determination of drugs surface tension and viscosity, spray geometry and size distribution of aerosol droplets, the topical delivery of each drug to different parts of the pediatric model of the nose with the flexible vestibule was evaluated by colorimetric visualization. All tested drugs are pseudo-plastic liquids, showing some differences in flow consistency constant k (range 714-1422) and flow behavior index n (range 0.16-0.31). At no-flow conditions, all sprays are deposited mainly in the anterior of the nasal cavity and the septum (2-3 cm from the nostril), as a result of inertial impaction of large droplets. The deposition range is slightly influenced by the geometry of the aerosol cloud, which, in turn, depends both on drug properties and the type of the spraying nozzle. Deposition experiments accompanied by the airflow show an enhancement of drug transport to deeper parts of the nasal cavity (up 4-6 cm from the vestibule), and this effect can be attributed to the secondary effects of spreading of the deposited liquid layer along the narrow air passages in the nose. Plume geometry, dose volume and rheological properties of the drug were shown to be important factors in the spray penetration pattern in the pediatric nose. The deepest delivery can be expected for drugs of low viscosity and short aerosol plumes.

Keywords: Deposition; Drug penetration; In vitro model; Mometasone; Nasal sprays.

MeSH terms

  • Administration, Intranasal / methods
  • Aerosols / chemistry*
  • Aerosols / metabolism*
  • Child
  • Humans
  • Mometasone Furoate / chemistry*
  • Nasal Cavity / drug effects*
  • Nasal Cavity / metabolism*
  • Nasal Sprays
  • Nebulizers and Vaporizers
  • Viscosity

Substances

  • Aerosols
  • Nasal Sprays
  • Mometasone Furoate