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Spray-freeze-drying aprepitant with hydroxypropyl cellulose increases nasal bioavailability.

Annika Rautenberg1, Paul Bühlbecker1, Jan Kožák1

  • 1Department of Pharmaceutics, Institute of Pharmacy, University of Bonn, Bonn, Germany.

International Journal of Pharmaceutics: X
|May 11, 2026
PubMed
Summary
This summary is machine-generated.

Spray-freeze-drying (SFD) with DMSO created amorphous aprepitant powders for nasal delivery. These SFD powders showed rapid dissolution and enhanced nasal bioavailability in rats compared to amorphous solid dispersions.

Keywords:
Amorphous solid particlesFast absorptionNasal aprepitantOrganic freeze-dryingPorous particlesSpray-freeze-drying

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Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Materials Science

Background:

  • Spray-freeze-drying (SFD) offers potential for novel drug formulations.
  • Nasal administration is an attractive route for therapeutic delivery.
  • Poorly water-soluble drugs present formulation challenges.

Purpose of the Study:

  • To investigate a non-aqueous SFD approach using dimethyl sulfoxide (DMSO).
  • To develop rapidly dissolving, amorphous aprepitant powders using hydroxypropyl cellulose (HPC) excipients.
  • To evaluate the nasal deposition and bioavailability of SFD-formulated aprepritant.

Main Methods:

  • Non-aqueous spray-freeze-drying (SFD) using DMSO as solvent.
  • Formulation of amorphous aprepitant powders with low-viscosity HPC grades (HPC-SSL, HPC-UL).
  • In vitro dissolution testing, nasal deposition studies, and in vivo pharmacokinetic evaluation in rats.

Main Results:

  • Spherical, porous, amorphous aprepitant particles (250-500 μm) were produced.
  • Rapid in vitro drug release (3 min) was achieved with aprepitant/HPC-UL (20/80 ratio), exceeding physical mixtures.
  • In vitro nasal deposition exceeded 90%; in vivo studies showed enhanced nasal bioavailability (at least threefold) compared to controls.

Conclusions:

  • Non-aqueous SFD is a viable method for producing amorphous drug powders for nasal delivery.
  • SFD formulations significantly improved aprepitant nasal bioavailability.
  • This platform holds promise for the nasal delivery of poorly water-soluble drugs.