Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2023 Oct 9:18:5685-5699.
doi: 10.2147/IJN.S430952. eCollection 2023.

Nasal Absorption Enhancement of Mometasone Furoate Nanocrystal Dispersions

Shuya Masuda #  1 , Saori Deguchi #  1 , Fumihiko Ogata  1 , Joji Yoshitomi  1 , Hiroko Otake  1 , Kazutaka Kanai  2 , Naohito Kawasaki  1 , Noriaki Nagai  1
Affiliations

Nasal Absorption Enhancement of Mometasone Furoate Nanocrystal Dispersions

Shuya Masuda et al. Int J Nanomedicine. .

Abstract

Purpose: We designed a 0.05% mometasone furoate (MF) nanocrystal dispersion and investigated whether the application of MF nanocrystals in nasal formulations enhanced local absorption compared to traditional nasal MF formulations (CA-MF).

Methods: MF nanocrystal dispersions (MF-NPs) were prepared by bead milling MF microcrystal dispersions (MF-MPs) consisting of MF, 2-hydroxypropyl-β-cyclodextrin, methylcellulose, and purified water. Pluronic F-127 combined with methylcellulose, Pluronic F-68, or carbopol was used as a base for in situ gelation (thickener). MF concentrations were measured using high-performance liquid chromatography, and nasal absorption of MF was evaluated in 6 week-old male Institute of Cancer Research (ICR) mice.

Results: The particle size range of MF prepared with the bead mill treatment was 80-200 nm, and the nanoparticles increased the local absorption of MF, which was higher than that of CA-MF and MF-MPs. In addition, unlike the results obtained in the small intestine and corneal tissue, the high absorption of nanocrystalline MF in the nasal mucosa was related to a pathway that was not derived from energy-dependent endocytosis. Moreover, the application of the in situ gelling system attenuated the local absorption of MF-NPs, owing to a decrease in drug diffusion in the dispersions.

Conclusion: We found that nanoparticulation of MF enhances local intranasal absorption, and nasal bioavailability is higher than that of CA-MF. In addition, we demonstrate that viscosity regulation is an important factor in the design of nasal formulations based on MF nanocrystals. These findings provide insights for the design of novel nanomedicines with enhanced nasal bioavailability.

Keywords: drug delivery; in situ gel; mometasone furoate; nanocrystal; nasal absorption.

PubMed Disclaimer

Conflict of interest statement

The authors report no conflicts of interest in this work.

Figures

None
Graphical abstract
Figure 1
Figure 1
Digital image (A) and particle size frequencies of commercially available mometasone furoate (CA-MF) (B), MF microcrystal dispersions (MF-MPs) (C), and MF nanocrystal dispersions (MF-NPs) (D).
Figure 2
Figure 2
Analysis of the crystal structures of MF in MF-MPs and MF-NPs.
Figure 3
Figure 3
Evaluation of the solubilities (A), membrane permeabilities (B), and dispersibilities (C and D) of CA-MF, MF-MPs, and MF-NPs.
Figure 4
Figure 4
Changes in the viscosities (A) and zeta potentials (B) of CA-MF, MF-MPs, and MF-NPs.
Figure 5
Figure 5
Changes in MF content in nasal mucosa of mice treated with CA-MF, MF-MPs and MF-NPs.
Figure 6
Figure 6
Changes in the particle size and viscosity of MF-NPs by the addition of a thickener.
Figure 7
Figure 7
Changes in MF contents (A) and AUC0-5h (B) in the nasal mucosa of mice treated with MF-NPs@F127/MC, MF-NPs@F127/F68, and MF-NPs@F127/Car.
Figure 8
Figure 8
Mechanism for nasal absorption after treatment with MF nanocrystals.
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

References

    1. Prenner BM, Schenkel E. Allergic rhinitis: treatment based on patient profiles. Am J Med. 2006;119(3):230–237. doi:10.1016/j.amjmed.2005.06.015 - DOI - PubMed
    1. Compalati E, Penagos M, Henley K, Canonica GW. Allergy prevalence survey by the World Allergy Organization. Allergy Clin Immunol Int J World Allergy Org. 2007;19:82–90.
    1. Asher MI, Montefort S, Bjӧrkstén B, et al. Worldwide time trends in the prevalence of symptoms of asthma, allergic rhinoconjunctivitis, and eczema in childhood: ISAAC Phases One and Three repeat multicountry cross-sectional surveys. Lancet. 2006;368(9537):733–743. doi:10.1016/S0140-6736(06)69283-0 - DOI - PubMed
    1. van Cauwenberge P, Bachert C, Passalacqua G, et al. Consensus statement on the treatment of allergic rhinitis. European Academy of Allergology and Clinical Immunology. Allergy. 2000;55(2):116–134. - PubMed
    1. Bousquet J, van Cauwenberge P, Khaltaev N, et al. Allergic rhinitis and its impact on asthma. J Allergy Clin Immunol. 2001;108(5 Suppl):S147–S334. - PubMed